Verapamil HCl

別名：CP-16533-1, (±)-Verapamil

製品コード：S4202 純度：99.98%

Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.Verapamil (CP-16533-1) HCl can be used to induce animal models of Heart Failure.

CAS No. 152-11-4

サイズ	価格(税別)	在庫状況
50mg	JPY 22000	国内在庫あり
1g	JPY 100500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（25）

カスタマーフィードバック3例

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Verapamil HCl関連製品

関連ターゲット	Cav 2.2	もっと見る
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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Ion Channel Ligand Library Exosome Secretion Related Compound Library Calcium Channel Blocker Library	もっと見る

シグナル伝達経路

Calcium Channelシグナル伝達経路

Calcium Channel阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
MCF7/VP	Function assay	20 uM	48 hrs	Inhibition of MRP expressed in human MCF7/VP cells assessed as increase in vincristine-induced cytotoxicity at 20 uM after 48 hrs by SRB binding assay	8786364
human MCF7/ADR cells	Function assay	10 μM	48 h	Inhibition of P-gp in human MCF7/ADR cells assessed as reversal of multidrug resistance at 10 uM by measuring EC50 for adriamycin-induced cytotoxicity after 48 hrs by SRB colorimetric assay, EC50=4.89 μM	25856545
KB-3-1	Cytotoxicity assay	5 uM	68 hrs	Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay, IC50=0.0047μM	17488128
KB-C2	Cytotoxicity assay	5 uM	68 hrs	Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-C2 cells at 5 uM after 68 hrs by MTT assay, IC50=0.1μM	17488128
MDCK2	Function assay	10 uM	40 mins	Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins	17964170
PC12	Autophagy assay	1 uM	24 hrs	Induction of autophagy in rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 1 uM after 24 hrs by densitometric analysis	18391949
PC12	Autophagy assay	1 uM	96 hrs	Induction of autophagy in rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as soluble EGFP-HDQ74 clearance at 1 uM after 96 hrs by densitometric analysis	18391949
SK-N-MC	Autophagy assay	1 uM	48 hrs	Induction of autophagy in human SK-N-MC cells expressing EGFP-HDQ74 assessed as reduction in EGFP-HDQ74 aggregation at 1 uM after 48 hrs by densitometric analysis	18391949
SK-N-MC	Autophagy assay	0.33 uM	24 hrs	Induction of autophagy in human SK-N-MC cells assessed as increase in LC3-2 level at 0.33 uM after 24 hrs by immunoblotting analysis	18391949
SK-N-MC	Autophagy assay	1 uM	48 hrs	Induction of autophagy in Atg positive human SK-N-MC cells expressing EGFP-HDQ74 at 1 uM after 48 hrs	18391949
PC12	Autophagy assay	1 uM	24 hrs	Induction of autophagy in pretreated rat stable inducible PC12 cells expressing EGFP-HDQ74 assessed as calpain activation at 1 uM followed by doxycyline treatment measured after 24 hrs	18391949
SK-N-SH	Autophagy assay	1 uM	48 hrs	Induction of autophagy in human SK-N-SH cells expressing EGFP-HDQ74 assessed as inhibition of Bay K8644-induced EGFP-HDQ74 aggregation at 1 uM after 48 hrs	18391949
RBMEC	Function assay	10 umol/L	90 mins	Inhibition of Pgp-mediated multidrug resistance activity in rat RBMEC cells assessed as Rh123 accumulation at 10 umol/L after 90 mins	18502125
K562	Function assay	1 uM	72 hrs	Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 1 uM after 72 hrs by MTT assay	19140665
K562	Function assay	3 uM	72 hrs	Potentiation of doxorubicin-induced growth inhibition in human doxorubicin-resistant K562 cells expressing Pgp at 3 uM after 72 hrs by MTT assay	19140665
MDCK	Function assay	30 uM	1.5 hrs	Inhibition of human MDR1 expressed in MDCK cells assessed as fluorescence activity at 30 uM after 1.5 hrs by rhodamine 123 efflux test	20363635
NIH-3T3	Function assay	10 uM	30 mins	Inhibition of human MDR1 expressed in mouse NIH-3T3 cells assessed as daunomycin efflux at 10 uM after 30 mins by flow cytometry	21856049
Caco2	Function assay	5 to 25 uM	1.5 hrs	Inhibition of P-glycoprotein overexpressed in human Caco2 cells assessed as increase in digoxin accumulation at 5 to 25 uM incubated for 1.5 hrs prior to digoxin treatment measured after 1.5 hrs by LC/MS/MS analysis	22209486
K562/A02	Function assay	10 uM	24 hrs	Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated for 24 hrs followed by adriamycin treated 6 hrs after drug washout by MTS assay, IC50=26.06μM	22405646
K562/A02	Function assay	0.25 to 5 after	60 mins	Inhibition of p-glycoprotein-mediated rhodamine 123 efflux in human K562/A02 cells at 0.25 to 5 after 60 mins by fluorescence microscopic analysis	22405646
K562/A02	Function assay	10 uM	30 mins	Inhibition of Pgp-mediated rhodamine 123 efflux in human K562/A02 cells assessed as intracellular rhodamine 123 accumulation at 10 uM preincubated for 30 mins measured after 60 mins by fluorescence microscopy relative to control	22429509
K562/A02	Function assay	10 uM	24 hrs	Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout before addition of adriamycin measured after 72 hrs by MTS assay (Rvb = 33.59 uM)	22429509
K562/A02	Function assay	10 uM	24 hrs	Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 6 hrs post washout measured after 72 hrs by MTS assay (Rvb = 35	22429509
K562/A02	Function assay	10 uM	24 hrs	Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 12 hrs post washout measured after 72 hrs by MTS assay (Rvb = 5	22429509
K562/A02	Function assay	10 uM	24 hrs	Inhibition of P-glycoprotein in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 10 uM preincubated for 24 hrs followed by washout addition of adriamycin at 24 hrs post washout measured after 72 hrs by MTS assay (Rvb = 5	22429509
K562/A02	Function assay	0.33 to 10 uM	60 mins	Inhibition of Pgp-mediated rhodamine-123 efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of rhodamine-123 at 0.33 to 10 uM after 60 mins by flow cytometry analysis	22450134
K562/A02	Function assay	0.33 to 10 uM	60 mins	Inhibition of Pgp-mediated rhodamine-123 efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of rhodamine-123 at 0.33 to 10 uM after 60 mins by fluorescence microscopic analysis	22450134
K562/A02	Function assay	0.33 to 10 uM	60 mins	Inhibition of Pgp-mediated adriamycin efflux in multidrug-resistance human K562/A02 cells assessed as increase in intracellular accumulation of adriamycin at 0.33 to 10 uM after 60 mins by FACS flow cytometry	22450134
KBVIN	Function assay	10 uM	72 hrs	Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as paclitaxel-induced cytotoxicity at 10 uM after 72 hrs by SRB assay	22612652
KBVIN	Function assay	10 uM	72 hrs	Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as vincristine-induced cytotoxicity at 10 uM after 72 hrs by SRB assay	22612652
KBVIN	Function assay	10 uM	72 hrs	Inhibition of P-gp-mediated multidrug-resistance in human KBVIN cells assessed as doxorubicin-induced cytotoxicity at 10 uM after 72 hrs by SRB assay	22612652
KB/VCR	Function assay	5 uM	72 hrs	Inhibition of p-gp in human KB/VCR cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM after 72 hrs by MTT assay	23683834
KB/VCR	Function assay	5 uM	72 hrs	Inhibition of p-gp in human KB/VCR cells assessed as potentiation of vincristine-induced cytotoxicity at 5 uM after 72 hrs by MTT assay	23683834
MDCK	Function assay	100 uM	2 hrs	Activation of ATPase activity of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction of reduction of ATP level at 100 uM after 2 hrs by luminescence/ATPlite assay	24607999
NCI-H292	Cytotoxicity assay	50 uM	72 hrs	Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=0.18μM	25215856
NCI-H292	Cytotoxicity assay	50 uM	72 hrs	Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=1.2μM	25215856
H460	Cytotoxicity assay	50 uM	72 hrs	Potentiation of erlotinib-induced cytotoxicity against human H460 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=10.3μM	25215856
H460/Vbl	Cytotoxicity assay	50 uM	72 hrs	Potentiation of erlotinib-induced cytotoxicity against human H460/Vbl cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=13.3μM	25215856
H460	Cytotoxicity assay	50 uM	72 hrs	Potentiation of gefitinib-induced cytotoxicity against human H460 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=19.6μM	25215856
H460/Vbl	Cytotoxicity assay	50 uM	72 hrs	Potentiation of gefitinib-induced cytotoxicity against human H460/Vbl cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=25.7μM	25215856
K562	Function assay	3 uM	72 hrs	Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562 cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.023 +/- 0.004 uM), IC50=0.029μM	25282263
K562/DOX	Function assay	3 uM	72 hrs	Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562/DOX cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 2.00 +/- 0.24 uM), IC50=0.74μM	25282263
K562/ADR	Function assay	10 uM	2.5 hrs	Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence microscopy	25462264
K562/ADR	Function assay	10 uM	2.5 hrs	Increase in adriamycin uptake in human K562/ADR cells at 10 uM after 2.5 hrs by fluorescence spectrophotometry	25462264
K562/ADR	Cytotoxicity assay	10 uM	48 hrs	Potentiation of adriamycin-induced cytotoxicity against human K562/ADR cells at 10 uM after 48 hrs by MTT assay	25462264
K562/A02	Function assay	5 uM	48 hrs	Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM after 48 hrs by MTT assay, IC50=6.8μM	25464884
K562/A02	Function assay	5 uM	24 hrs	Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs prior to adriamycin treatment measured after 48 hrs by MTT assay, IC50=9.6μM	25464884
K562/A02	Function assay	2.5 uM	48 hrs	Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay, IC50=15.92μM	25464884
K562/A02	Function assay	5 uM	24 hrs	Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as reduction of adriamycin IC50 at 5 uM incubated for 24 hrs followed by adriamycin treatment post compound washout measured after 48 hrs by MTT assay, IC50=40.8μM	25464884
KB/VCR	Cytotoxicity assay	25 uM	72 hrs	Cytotoxicity against human KB/VCR cells assessed as vincristine IC50 at 25 uM after 72 hrs by SRB method, IC50=0.02μM	25597010
K562/R7	Cytotoxicity assay	1 uM	72 hrs	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.6μM	25634041
MDA435/LCC6MDR	Function assay	1 uM	5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 1 uM after 5 days by CellTiter 96 Aqueous assay, IC50=0.038μM	25985195
MDA435/LCC6MDR	Function assay	3 uM	150 mins	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as restoration of intracellular doxorubicin accumulation at 3 uM after 150 mins by spectrofluorometric analysis relative to parental cells	25985195
MCF7/D70	Function assay	10 uM	72 hrs	Inhibition of P-gp in human MCF7/D70 cells assessed as decrease in doxorubicin IC50 at 10 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.906 +/- 0.02 uM), IC50=0.2μM	26840362
K562/A02	Function assay	5 uM	48 hrs	Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM), IC50=8.5μM	27073052
K562/A02	Function assay	2.5 uM	48 hrs	Reversal of P-gp-mediated resistance to adriamycin in human K562/A02 cells assessed as adriamycin IC50 at 2.5 uM after 48 hrs by MTT assay (Rvb = 38.02 +/- 1.65 uM), IC50=19.84μM	27073052
MDA435/LCC6MDR	Function assay	1 uM	5 days	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM), IC50=0.0351μM	27750197
K562	Function assay	10 uM	1 hr	Inhibition of P-gp in doxorubicin resistant human K562 cells assessed as increase in accumulation of rhodamine 123 at 10 uM measured after 1 hr by flow cytometry	27908756
K562/A02	Function assay	0.33 to 10 uM	1 hr	Inhibition of P-gp in human K562/A02 cells assessed as increase in intracellular rhodamine123 accumulation at 0.33 to 10 uM measured after 1 hr by flow cytometry	28068095
LoVo/DX	Function assay	2.5 to 10 uM	15 mins	Inhibition of P-gp in human LoVo/DX cells assessed as reduction in Rhodamine123 efflux at 2.5 to 10 uM preincubated for 15 mins followed by Rhodamine123 addition measured after 1 hr by flow cytometry	28109950
LoVo/DX	Function assay	10 uM	2 hrs	Substrate activity at P-gp in human LoVo/DX cells assessed as ATP consumption at 10 uM after 2 hrs by ATPlite assay	28109950
MCF7/DX	Function assay	5 uM	48 hrs	Reversal of multidrug resistance in human MCF7/DX cells assessed as potentiation doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 level at 5 uM incubated for 48 hrs by MTT assay, IC50=6.59μM	28245113
K562/A02	Function assay	5 uM	2.5 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular adriamycin accumulation at 5 uM after 2.5 hrs by spectrofluorimetric analysis	28301155
K562/A02	Function assay	5 uM	up to 90 mins	Inhibition of ABCB1 in human K562/A02 cells assessed as increase in intracellular Rh123 accumulation at 5 uM up to 90 mins by flow cytometry	28301155
K562/A02	Function assay	5.0 uM	up to 90 mins	Inhibition of P-gp mediated efflux in human K562/A02 cells assessed as intracellular Rh123 accumulation at 5.0 uM measure up to 90 mins by flow cytometric analysis	28355069
K562/A02	Function assay	5 uM	24 hrs	Inhibition of P-gp in human K562/A02 cells assessed as potentiation of doxorubicin-induced cytotoxicity at 5 uM preincubated for 24 hrs followed by doxorubicin addition measured after 48 hrs by MTT assay	28355069
K562/A02	Function assay	5.0 uM	150 mins	Inhibition of P-gp in human K562/A02 cells assessed as accumulation of doxorubicin at 5.0 uM after 150 mins by fluorescence spectrophotometric analysis	28355069
K562/A02	Function assay	5 uM	48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM), IC50=17.55μM	28645831
K562/A02	Function assay	0.5 to 2.5 uM	60 mins	Inhibition of ABCB1 in human K562/A02 cells assessed as increase in adriamycin accumulation at 0.5 to 2.5 uM pretreated for 60 mins followed by ADR addition after 90 mins by fluorescence spectrophotometric method	28645831
SW620/AD300	Function assay	2 uM	30 to 120 mins	Inhibition of ABCB1 in human SW620/AD300 cells assessed as reduction in Rh123 efflux at 2 uM treated followed by Rh123 addition in Rh123 free medium for 30 to 120 mins by flow cytometry	29126726
MCF7/ADR	Function assay	10 uM	4 hrs	Inhibition of P-gp mediated efflux in human MCF7/ADR cells at 10 uM after 4 hrs by Rh123 dye-based flow cytometric method	29407947
K562/A02	Function assay	5 uM	2.5 hrs	Inhibition of P-gp in human K562/A02 cells assessed as increase in adriamycin accumulation at 5 uM after 2.5 hrs by flow cytometry method	29631786
K562	Function assay	5 uM	2.5 hrs	Inhibition of P-gp in human K562 cells assessed as increase in Rh123 accumulation at 5 uM after 2.5 hrs by by flow cytometry method	29631786
MCF7/ADR	Function assay	10 uM	2 hrs	Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular Rh123 accumulation at 10 uM after 2 hrs by flow cytometry	29903663
MCF7	Cytotoxicity assay	10 ug/ml	48 hrs	Potentiation of adriamycin-induced cytotoxicity in human MCF7 cells assessed as adriamycin IC50 at 10 ug/ml after 48 hrs by MTT assay (Rvb = 1.3 +/- 0.2 uM), IC50=1.5μM	30137985
MCF7/ADR	Function assay	10 ug/ml	24 hrs	Inhibition of P-gp in human MCF7/ADR cells assessed as increase in intracellular accumulation of adriamycin by measuring increase in fluorescence intensity at 10 ug/ml after 24 hrs by fluorescence microscopic analysis	30137985
KBV	Function assay	10 uM	72 hrs	Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 1353.98 +/- 303.33 nM), IC50=0.02816μM	30347326
KBV	Function assay	10 uM	2 hrs	Inhibition of P-gp-mediated Rh-123 efflux in human KBV cells assessed as Rh-123 accumulation at 10 uM preincubated for 2 hrs followed by Rh-123 addition measured after 30 mins by flow cytometry	30347326
KBV	Function assay	10 uM	72 hrs	Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=6.15μM	30384042
KBV	Cytotoxicity assay	10 uM	48 hrs	Potentiation of vincristine-induced cytotoxicity against human KBV cells assessed as vincristine IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 666.3 nM), IC50=0.00131μM	30455148
A2780/TAX	Cytotoxicity assay	10 uM	48 hrs	Potentiation of paclitaxel-induced cytotoxicity against human A2780/TAX cells assessed as paclitaxel IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 3970 nM), IC50=0.0188μM	30455148
A2780/CDDP	Cytotoxicity assay	10 uM	48 hrs	Potentiation of cisplatin-induced cytotoxicity against human A2780/CDDP cells assessed as cisplatin IC50 at 10 uM after 48 hrs by MTT assay (Rvb = 43.11 nM), IC50=0.04011μM	30455148
Lucena 1	Function assay	12.5 uM	1 hr	Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 12.5 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry	30613324
Lucena 1	Function assay	25 uM	1 hr	Inhibition of P-gp-mediated Rho-123 efflux in human Lucena 1 cells at 25 uM preincubated for 1 hr followed by Rho-123 addition measured after 1 hr by flow cytometry	30613324
MCF7/ADR	Antiproliferative assay	5 uM	48 hrs	Potentiation of adriamycin-induced antiproliferative activity against human MCF7/ADR cells assessed as adriamycin IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 89.14 +/- 4.89 uM), IC50=2.25μM	30837097
MCF7/Dox	Function assay	12.5 uM	48 hrs	Reversal of P-gp-mediated multidrug resistance in human MCF7/Dox cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 12.5 uM after 48 hrs by MTT assay (Rvb = 51.19 +/- 0.95 microM), IC50=10.1μM	31325783
KBtax	Function assay	100 uM	1 hr	Inhibition of P-gp efflux in human KBtax cells at 100 uM after 1 hr by flow cytometry	31419740
KBV	Function assay	10 uM	72 hrs	Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 352.31 +/- 10.9 nM), IC50=0.01843μM	31505451
KBV	Function assay	10 uM	72 hrs	Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of vincristine-induced cytotoxicity by measuring vincristine IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 2.92 +/- 0.31 nM), IC50=0.03502μM	31505451
KBV	Function assay	10 uM	72 hrs	Reversal of P-gp-mediated multidrug resistance in human KBV cells assessed as potentiation of irinotecan-induced cytotoxicity by measuring irinotecan IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 49.2 +/- 0.46 nM), IC50=10.37μM	31505451
HepG2/Dox	Function assay	10 uM	4 hrs	Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular doxorubicin accumulation at 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by fluorescence microscopic analy	31585275
HepG2/Dox	Function assay	10 uM	4 hrs	Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by fluorescence microscopic analysis	31585275
HepG2/Dox	Function assay	5 to 10 uM	4 hrs	Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular doxorubicin accumulation at 5 to 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by flow cytometry analysis	31585275
HepG2/Dox	Function assay	5 to 10 uM	4 hrs	Reversal of P-gp mediated drug efflux in human HepG2/Dox cells assessed as increase in intracellular Rhodamine123 accumulation at 5 to 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by flow cytometry analysis	31585275
MCF7/ADM	Function assay	10 uM	4 hrs	Reversal of P-gp mediated drug efflux in human MCF7/ADM cells assessed as increase in intracellular doxorubicin accumulation at 10 uM preincubated for 4 hrs followed by doxorubicin addition measured after 1 hr incubation by fluorescence microscopic analys	31585275
MCF7/ADM	Function assay	10 uM	4 hrs	Reversal of P-gp mediated drug efflux in human MCF7/ADM cells assessed as increase in intracellular Rhodamine123 accumulation at 10 uM preincubated for 4 hrs followed by Rh123 addition measured after 1 hr incubation by fluorescence microscopic analysis	31585275
HepG2/Dox	Function assay	5 to 10 uM	4 hrs	Inhibition of P-gp mediated doxorubicin efflux in human HepG2/Dox cells at 5 to 10 uM preincubated for 4 hrs followed by co-incubation with doxorubicin for 2 hrs followed by doxorubicin wash-out and measured after 120 mins incubation with drug containing	31585275
MCF7/ADM	Function assay	5 to 10 uM	4 hrs	Inhibition of P-gp mediated doxorubicin efflux in human MCF7/ADM cells at 5 to 10 uM preincubated for 4 hrs followed by co-incubation with doxorubicin for 2 hrs followed by doxorubicin wash-out and measured after 120 mins incubation with drug containing c	31585275
K562/ADR	Function assay	10 to 20 uM	30 mins	Inhibition of P-glycoprotein in human K562/ADR cells at 10 to 20 uM after 30 mins by rhodamine 123 staining-based fluorescence assay	ChEMBL
K562	Function assay	10 to 20 uM	1 hr	Inhibition of P-glycoprotein in doxorubicin-resistant Homo sapiens (human) K562 cells overexpressing P-gp assessed as increase in intracellular Rh123 accumulation at 10 to 20 uM after 1 hr by flow cytometric analysis	ChEMBL
HCT116/VM46 cell	Function assay	1 μM		Effect on vinblastine IC50 against MDR human carcinoma HCT116/VM46 cell line at a dose of 1 uM concentration, IC50=0.004 μM	12729663
HCT15	Function assay	0.8 to 12.5 ug/mL		Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL	11754602
UO31	Function assay	0.8 to 12.5 ug/mL		Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL	11754602
CAKI1	Function assay	0.8 to 12.5 ug/mL		Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.8 to 12.5 ug/mL	11754602
BHK21	Cytotoxicity assay	10 to 20 uM		Cytotoxicity against human MRP1 expressing hamster BHK21 cells at 10 to 20 uM by MTT assay	17646169
Caco-2	Function assay	100 uM		Activation of human P-glycoprotein ATPase in Caco-2 cells assessed as ATP depletion at 100 uM	18257545
PC12	Autophagy assay	1 uM		Induction of autophagy in differentiated rat stable inducible PC12 cells assessed as increase in LC3-2 level cell pretreated at 1 uM in presence of 400 nM bafilomycin A1	18391949
HCT15	Function assay	40 uM		Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 40 uM by fluorescence assay	21348461
K562/A02	Function assay	10 uM		Reversal of p-glycoprotein-mediated multidrug-resistant in human K562/A02 cells assessed as increase of adriamycin-induced cytotoxic effect at 10 uM treated 24 hrs before adriamycin challenge followed by drug washout by MTS assay, IC50=12.92μM	22405646
A549/CDDP	Function assay	1.2 uM		Inhibition of P-gp in human A549/CDDP cells assessed as accumulation of rhodamine 123 at 1.2 uM by flow cytometry	26891099
KBV	Function assay	10 uM		Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 10 uM, IC50=0.0049μM	30384042
HepG2/DOX	Function assay	10 uM		Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay (Rvb = 69.3 +/- 3.9 uM), IC50=1.3μM	31585275
MCF7/ADM	Function assay	10 uM		Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as doxorubicin IC50 at 10 uM measured within 48 hrs by MTT assay (Rvb = 151.7 +/- 5 uM), IC50=3.7μM	31585275
HepG2/DOX	Function assay	5 uM		Reversal of P-gp mediated multidrug resistance in human HepG2/DOX cells assessed as doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay (Rvb = 69.3 +/- 3.9 uM), IC50=4.7μM	31585275
MCF7/ADM	Function assay	5 uM		Reversal of P-gp mediated multidrug resistance in human MCF7/ADM cells assessed as doxorubicin IC50 at 5 uM measured within 48 hrs by MTT assay (Rvb = 151.7 +/- 5 uM), IC50=17.8μM	31585275
KB31	Cytotoxicity assay		48 hrs	Cytotoxicity against human KB31 cells after 48 hrs by SRB method, IC50=45.2μM	10346948
KBV1	Cytotoxicity assay		48 hrs	Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs by SRB method, IC50=39.2μM	10346948
KBV1	Cytotoxicity assay		48 hrs	Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method, IC50=1.6μM	10346948
KB/MDR	Function assay		1 h	Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h, EC50=14μM	15481991
Caco-2	Antiproliferative assay		48 hrs	Antiproliferative activity against human Caco-2 cells assessed as cell viability by MTT assay after 48 hrs, IC10=24.9μM	17276076
CEM/VLB500	Function assay		3 days	Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay, EC50=1.041μM	17399990
A2780	Function assay		30 mins	Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay, IC50=4.57088μM	18083034
A2780	Function assay		30 mins	Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50=6.60693μM	18083034
MDCK2	Function assay		20 mins	Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins, EC50=5.1μM	18849167
MDCK2	Function assay		20 mins	Inhibition of human MDR1 expressed in MDCK2 cells assessed as enhancement of Calcein-AM uptake treated 30 mins before Calcein-AM challenge measured after 20 mins, IC50=14μM	19402665
2008/MRP1	Function assay		120 mins	Reversal of MRP1-mediated doxorubicin resistance in doxorubicin co-incubated human 2008/MRP1 cells assessed as minimum concentration required for restoration of doxorubicin accumulation after 120 mins by spectrofluorimetry relative to accumulation in huma	19725578
BHK21	Cytotoxicity assay		96 hrs	Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay, IC50=10.6μM	20691599
MDCK	Function assay		30 mins	Inhibition of human MDR1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay, IC50=0.5μM	22112208
MDCK	Function assay		30 mins	Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay, IC50=6.8μM	22112208
LCC6MDR	Function assay		5 days	Reversal of P-gp-mediated doxorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.245μM	22320402
LCC6MDR	Function assay		5 days	Reversal of P-gp-mediated vincristine-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.385μM	22320402
LCC6MDR	Function assay		5 days	Reversal of P-gp-mediated paclitaxel-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.428μM	22320402
LCC6MDR	Function assay		5 days	Reversal of P-gp-mediated vinblastin-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.503μM	22320402
MDA435/LCC6MDR	Function assay		150 mins	Inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin after 150 mins by fluorescence spectrophotometric analysis, MIC=8μM	22320402
CCRF-CEM/VCR1000	Function assay		240 secs	Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50=0.57544μM	22452412
BHK	Function assay		30 mins	Induction of ATPase activity of human His10-tagged P-gp expressed in BHK cells assessed as inorganic phosphate release after 30 mins by Michaelis-Menten analysis, Km=24μM	22533905
C1-6-37-3	Function assay		30 mins	Inhibition of human voltage-dependent L-type calcium channel subunit alpha1C/alpha2delta/beta2a expressed in C1-6-37-3 cells assessed as inhibition of K+-induced calcium influx incubated for 30 mins prior to K+-induction by Fluo-4-AM based FLIPR assay, IC50=0.9μM	22694270
KB/VCR	Function assay		72 hrs	Inhibition of p-gp in human KB/VCR cells assessed as potentiation of 100 nM docetaxel-induced cytotoxicity after 72 hrs by MTT assay, EC50=1.253μM	23683834
MDCK	Function assay		30 mins	Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay, EC50=20μM	24607999
NCI/ADR-RES	Function assay		20 mins	Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay	24992153
MDCK	Function assay		30 mins	Inhibition of MRP1 (unknown origin) expressed in MDCK cells after 30 mins by Calcein-AM assay, IC50=3.5μM	25093931
A7R5	Function assay		15 mins	Antagonist activity at calcium channel in rat A7R5 cells assessed as inhibition of Cacl2/KCl-induced increase in intracellular Ca2+ incubated for 15 mins prior to Cacl2/KCl challenge by fluorescence assay, IC50=0.3μM	25311564
MES-SA	Function assay		15 mins	Modulation of P-gp mediated drug efflux in human MES-SA cells assessed as accumulation of rhodamine-123 incubated for 15 mins prior to rhodamine-123 addition measured after 1 hr by fluorescence analysis, EC50=7.1μM	25311564
H69	Function assay		15 mins	Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis, EC50=27.8μM	25311564
MES-SA	Function assay		15 mins	Modulation of BCRP1 mediated drug efflux in mitoxantrone-resistant human MES-SA cells assessed as accumulation of hoechst 33342 incubated for 15 mins prior to rhodamine-123 addition measured after 90 mins by fluorescence analysis, EC50=37.3μM	25311564
MDA435/LCC6MDR	Function assay		5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing doxorubicin resistance measured as cell survival after 5 days by MTS assay, EC50=0.245μM	25985195
MDA435/LCC6MDR	Function assay		5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing vincristine resistance measured as cell survival after 5 days by MTS assay, EC50=0.385μM	25985195
MDA435/LCC6MDR	Function assay		5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay, EC50=0.446μM	25985195
MDA435/LCC6MDR	Function assay		5 days	Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing vinblastine resistance measured as cell survival after 5 days by MTS assay, EC50=0.503μM	25985195
KB/VJ300	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB/VJ300 cells assessed as cell viability after 72 hrs by MTT assay in presence of 0.121 uM vincristine, IC50=10.3μM	26717050
KB/VJ300	Growth inhibition assay		72 hrs	Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay, IC50=4.6μM	26918761
L5178Y	Cytotoxicity assay		72 hrs	Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=47.85μM	27156771
HLF	Cytotoxicity assay		48 hrs	Cytotoxicity against HLF cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=27.18μM	27328029
MDA435/LCC6MDR	Function assay		5 days	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of doxorubicin cytotoxic IC50 by half after 5 days by Cell Titer 96 Aqueous assay, EC50=0.245μM	27750197
MDA435/LCC6MDR	Function assay		150 mins	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as increase in doxorubicin accumulation to half of parental LCC6 cells measured after 150 mins by fluorescence spectrophotometric method, EC50=0.35μM	27750197
MDA435/LCC6MDR	Function assay		5 days	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vincristine cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay, EC50=0.385μM	27750197
MDA435/LCC6MDR	Function assay		5 days	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of paclitaxel cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay, EC50=0.446μM	27750197
MDA435/LCC6MDR	Function assay		5 days	Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as reduction of vinblastine cytotoxic IC50 by half measured after 5 days by Cell Titer 96 Aqueous assay, EC50=0.503μM	27750197
MES-SA/Dx5	Function assay		72 hrs	Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring compound concentration required for reduction of doxorubicin IC50 by half after 72 hrs by MTT assay, EC50=0.7μM	28043777
MES-SA/Dx5	Function assay		72 hrs	Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring compound concentration required for reduction of paclitaxel IC50 by half after 72 hrs by MTT assay, EC50=0.8μM	28043777
MES-SA/Dx5	Function assay		72 hrs	Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of actinomycin D-induced cytotoxicity by measuring compound concentration required for reduction of actinomycin D IC50 by half after 72 hrs by MTT assay, EC50=0.9μM	28043777
MES-SA/Dx5	Function assay		72 hrs	Inhibition of P-gp in human MES-SA/Dx5 cells assessed as potentiation of vinblastine-induced cytotoxicity by measuring compound concentration required for reduction of vinblastine IC50 by half after 72 hrs by MTT assay, EC50=1μM	28043777
K562/DOX	Function assay		30 mins	Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by spectroflurometry, I0.5=1.6μM	28113128
K562/A02	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562/A02 cells overexpressing P-gp after 48 hrs by MTT assay, IC50=31.28μM	28301155
K562	Cytotoxicity assay		48 hrs	Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=36.7μM	28301155
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=10.73μM	28645831
K562/A02	Function assay		48 hrs	Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=31.28μM	28645831
MCF7/ADR	Function assay		48 hrs	Inhibition of P-gp in human MCF7/ADR cells assessed as potentiation of doxorubicin-induced cytotoxicity after 48 hrs by MTT assay, EC50=0.2451μM	29407947
MCF7/ADR	Function assay		150 mins	Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Lineweaver-Burk plot analysis, Ki=2.88μM	29407947
MCF7/ADR	Function assay		150 mins	Competitive inhibition of P-gp in human MCF7/ADR cells after 150 mins in presence of doxorubicin by Dixon plot analysis, Ki=2.92μM	29407947
MCF7/ADR	Function assay		150 mins	Inhibition of P-gp in human MCF7/ADR cells assessed as concentration required to restore doxorubicin accumulation in cells after 150 mins by fluorescence assay relative to MCF7 cells, Activity=40μM	29407947
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=48.91μM	29407947
MCF7/ADR	Function assay		48 hrs	Inhibition of P-gp in human MCF7/ADR cells assessed as cell viability after 48 hrs by MTT assay, EC50=20.54μM	29656198
KB/VJ300	Growth inhibition assay		72 hrs	Growth inhibition of human KB/VJ300 cells after 72 hrs in presence of 0.1 uM of vincristine by MTT assay, IC50=0.1μM	29746134
SW620/AD300	Function assay		2 hrs	Inhibition of ABCB1 in human SW620/AD300 cells assessed as intracellular accumulation of paclitaxel up to 2 uM treated at 2 hrs post paclitaxel treatment for 30 mins in paclitaxel free medium by HPLC analysis	29975529
SW620/AD300	Function assay		4 hrs	Inhibition of ABCB1 in human SW620/AD300 cells assessed as decrease in rhodamine 123 efflux up to 2 uM preincubated for 4 hrs followed by 30 mins incubation in Rho-123 containing medium and subsequent incubation in Rho-123 free medium up to 120 mins by fl	29975529
SW620/AD300	Function assay		4 hrs	Inhibition of ABCB1 in human SW620/AD300 cells assessed as intracellular accumulation of [3H]-paclitaxel up to 2 uM preincubated for 4 hrs followed by [3H]-paclitaxel addition measured after 2 hrs by liquid scintillation counting method	29975529
2008/MRP1	Function assay		5 days	Inhibition of MRP1 in human 2008/MRP1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring reduction in cell survival after 5 days by MTS assay, EC50=1.925μM	30351934
MDCK	Function assay		30 mins	Inhibition of MDR1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method, IC50=1.3μM	30384046
MDCK	Function assay		30 mins	Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured after 30 mins by spectrofluorimetric method, IC50=4.5μM	30384046
MCF7/ADR	Function assay		48 hrs	Inhibition of P-gp in doxorubicin-resistant human MCF7/ADR cells assessed as reversal of doxorubicin resistance by measuring doxorubicin IC50 incubated for 48 hrs by MTT assay (Rvb = doxorubicin alone = 64.8 +/- 2.1 uM), IC50=4.7μM	30860373
KB/VJ300	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB/VJ300 cells after 72 hrs in presence of vincristine by MTT assay, IC50=0.8μM	30869890
MDCK-MDR1	Function assay		30 mins	Inhibition of P-gp (unknown origin) expressed in MDCK-MDR1 cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay, EC50=0.5μM	31494468
MDCK	Function assay		30 mins	Inhibition of BCRP (unknown origin) expressed in MDCK cells assessed as increase in Hoechst 33342 accumulation incubated for 30 mins by Hoechst 33342 dye based fluorescence assay, EC50=0.9μM	31494468
K562/DOX	Function assay		30 mins	Inhibition of P-gp in human K562/DOX cells assessed as drug level causing 50% increase in nuclear pirarubicin concentration incubated for 30 mins by fluorescence based assay, I0.5=1.6μM	31494468
MDCK	Function assay		30 mins	Inhibition of MRP1 (unknown origin) expressed in MDCK cells assessed as increase in calcein-AM accumulation incubated for 30 mins by calcein-AM dye based fluorescence assay, EC50=6.8μM	31494468
KB/VJ300	Antiproliferative assay		72 hrs	Antiproliferative activity against human vincristine-rsistant KB/VJ300 cells assessed as reduction in cell growth after 72 hrs by MTT assay, IC50=0.4μM	31642315
HeLa	Function assay		30 mins	Inhibition of P-glycoprotein 1 in human HeLa cells assessed as intracellular accumulation of Hoechst 33342 dye after 30 mins by fluorescence microscopic analysis, IC50=1.7μM	ChEMBL
HEK293	Function assay		24 hrs	Inhibition of Marburg virus envelope glycoprotein-mediated cell entry in rVSIV-deltaG-MarV-GP pseuotype virus infected HEK293 cells after 24 hrs post transfection by luciferase reporter gene assay, IC50=13μM	ChEMBL
NIH-3T3-G185	Function assay			TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50=6.5μM	11716514
NIH-3T3-G185	Function assay			TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=4.7μM	11716514
NIH-3T3-G185	Function assay			TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50=4.2μM	11716514
G185	Function assay			TP_TRANSPORTER: inhibition of Daunorubicin efflux (Daunorubicin: ? uM) in G185 cells, IC50=4.2μM	11454724
Caco-2	Function assay			TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells, Ki=3μM	11405287
Caco-2	Function assay			TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells, IC50=2.1μM	10820137
P388	Function assay			Multidrug-resistant reversal activity using P388/VMDRC.04 cells (a subline of P388 murine leukemia cells expressing human recombinant human P-glycoprotein) in the presence of 10 nM vincristine, IC50=3.1μM	10386932
S1-B1-20	Function assay			In vitro concentration required to inhibit tumor activity on subclone of human colon carcinoma cells (S1-B1-20) resistant to bisantrene, IC50=17.27μM	10377220
K562/DOX MDR	Cytotoxicity assay			Ability to potentiate DOX cytotoxicity on K562/DOX MDR cells. Cell survival was assayed by MTT conversion, IC50=37μM	9986718
HeLa	Function assay			TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing HeLa cells, Ki=2.9μM	9655880
B16/F10	Function assay			Inhibition of human MDR1 expressed in mouse B16/F10 cells assessed as increase in doxorubicin accumulation by fluorimetry, ED50=3μM	9461658
MCF/ADR	Function assay			Reversal of P-gp-mediated multidrug resistance in human MCF/ADR cells assessed as increase in rhodamine 6G accumulation	8984151
CCRF-CEM	Function assay			The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM etoposide, ED50=3.4μM	7629817
CCRF-CEM	Function assay			The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin, ED50=0.045μM	7629817
NG108-15	Function assay			The compound was tested for inhibition of calcium influx into neuronal (NG108-15) cells, IC50=6.5μM	2033584
NIH-3T3-G185	Function assay			TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells, IC50=28.9μM	11716514
NIH-3T3-G185	Function assay			TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells, IC50=38.2μM	11716514
NIH-3T3-G185	Function assay			TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells, IC50=42μM	11716514
MDA-435/LCC6 and MDA-435/LCC6-MDRI cells	Function assay			Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%, EC50=1.2μM	11784143
MDA-435/LCC6 and MDA-435/LCC6-MDRI cells	Function assay			Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%., EC50=2.4μM	11784143
MDA-435/LCC6	Function assay			Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50=3.1μM	11784143
MDA435/LCC6 MDR1	Function assay			TP_TRANSPORTER: reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells, EC50=3.1μM	11784143
MDA-435/LCC6	Function assay			Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50=4.1μM	11784143
BTI-TN5B1-4	Function assay			TP_TRANSPORTER: ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km=4.06μM	11785684
MDCK	Function assay			TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells, Ki=15.1μM	12134945
human embryonic kidney cells	Function assay			K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1, IC50=0.143μM	12190308
HCT15/CL02	Function assay			TP_TRANSPORTER: drug resistance (paclitaxel) in HCT15/CL02 cells, IC50=2.21μM	12569305
MES-SA/DX5	Function assay			TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells, IC50=4.78μM	12569305
Caco-2	Function assay			TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells, Ki=0.88μM	12636153
L-MDR1	Function assay			TP_TRANSPORTER: cell accumulation of calcein in L-MDR1 cells, IC50=18.9μM	12649369
LLC-PK1	Function assay			Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=2μM	12699389
LLC-PK1	Function assay			TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells, IC50=2μM	12699389
LLC-PK1	Function assay			Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=6.3μM	12699389
LLC-PK1	Function assay			TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells, IC50=6.3μM	12699389
LLC-PK1	Function assay			Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=10μM	12699389
LLC-PK1	Function assay			TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells, IC50=10μM	12699389
CHO	Function assay			Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1, IC50=0.143μM	12729675
mammalian cells	Function assay			Inhibition of human Potassium channel HERG expressed in mammalian cells, IC50=0.14125μM	12873512
AML-2/D100	Function assay			TP_TRANSPORTER: drug resistance (vincristine) in AML-2/D100 cells, IC50=0.4μM	15240100
Caco-2	Function assay			TP_TRANSPORTER: transepithelial transport of fexofenadine in Caco-2 cells, IC50=8.44μM	15359574
Sf9	Function assay			Michaelis-Menten constant for human P-glycoprotein expressed in Sf9 cells, Km=2μM	15863325
K562	Function assay			Reversal of P-gp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug concentration causing half-maximal increase in nuclear pirarubicin concentration, Activity=1.6μM	16279802
Caco-2	Function assay			Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=20μM	17064079
MDA435/LCC6	Function assay			Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, IC50=0.00025μM	17154505
MDA435/LCC6	Function assay			Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, IC50=0.0052μM	17154505
MDA435/LCC6	Function assay			Reversal of paclitaxel resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, EC50=0.7μM	17154505
K562	Function assay			Inhibition of human Pgp in anthracycline-resistant K562 cells assessed as drug level causing half maximal increase in nuclear concentration of pirarubicin, Activity=1.6μM	17256837
A549	Function assay			Inhibition of P-gp in A549 cells assessed as drug concentration required to double baseline fluorescence level by calcein-AM uptake assay, Activity=7μM	17419606
THP1	Antileishmanial assay			Antileishmanial activity against wild-type Leishmania amazonensis MHOM/BR/1973/MM2269 promastigotes infected in human THP1 cells by luciferase based assay, IC50=19.1μM	17452480
THP1	Antileishmanial assay			Antileishmanial activity against wild-type Leishmania major LV39 promastigotes infected in human THP1 cells by luciferase based assay, IC50=40.3μM	17452480
THP1	Antileishmanial assay			Antileishmanial activity against wild-type Leishmania infantum MHOM/MA/67/ITMAP-263 promastigotes infected in human THP1 cells by luciferase based assay, IC50=43.2μM	17452480
BHK21	Function assay			Inhibition of human MRP1 mediated LTC4 transport in hamster BHK21 cells in presence of glutathione by rapid filtration technique	17646169
A2780/ADR	Function assay			Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50=4.57088μM	17890094
Caco-2	Function assay			Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells, EC50=20μM	17936633
Caco-2	Function assay			Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells, EC50=20μM	18257545
Caco-2	Function assay			Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells, EC50=20μM	18276145
KBV20C	Cytotoxicity assay			Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of paclitaxel by MTS assay, IC50=0.01μM	18295490
KBV20C	Cytotoxicity assay			Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of vincristine by MTS assay, IC50=0.2μM	18295490
KBV20C	Function assay			Inhibition of Pgp in multidrug resistant human KBV20C cells assessed as increase in intracellular accumulation of Rh123	18295490
K562	Function assay			Activity of Pgp-ATPase in doxorubicin-resistant human K562 cells, Km=0.7μM	18313307
K562	Function assay			Inhibition of Verapamil-stimulated human Pgp-ATPase activity in doxorubicin-resistant K562 cells, Km=0.89μM	18313307
K562	Function assay			Inhibition of Verapamil-stimulated human Pgp-ATPase activity in doxorubicin-resistant K562 cells, Vmax=22.39μM	18313307
K562	Function assay			Activity of Pgp-ATPase in doxorubicin-resistant human K562 cells, Vmax=36.93μM	18313307
CHO	Function assay			Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.14125μM	18448342
Caco-2	Function assay			Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells, EC50=20μM	18524592
A2780	Function assay			Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=4.57088μM	18678495
A2780	Function assay			Inhibition of P-gp in human A2780 cells, IC50=5.42μM	18707884
2008	Function assay			Inhibition of human MRP1 in human 2008 cells, IC50=9.66μM	18707884
HEK293	Function assay			Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy, IC50=6.8μM	18788725
MCF7	Function assay			Inhibition of human ERG in MCF7 cells, IC50=0.14454μM	19110341
K562	Function assay			Reversal of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing maximum increase in nuclear concentration of pirarubicin by spectrofluorimetry relative to control, Alpha max=0.7μM	19140665
K562	Function assay			Reversal of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing 50% increase in nuclear concentration of pirarubicin by spectrofluorimetry, Activity=1.6μM	19140665
smooth skeletal cells	Function assay			Displacement of (-)-[3H]devapamil from L-type calcium channel in rabbit smooth skeletal cells relative to verapamil, IC50=0.0602μM	19203272
A2780/ADR	Function assay			Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50=5.2μM	19250834
BHK	Function assay			Induction of human histidine10-tagged MDR1 ATPase activity expressed in BHK cells by apparent Michaelis-Menten constant, Km=24μM	19402665
2008/MRP1	Function assay			Reversal of MRP1-mediated doxorubicin-resistance in human 2008/MRP1 cells assessed as reduction of doxorubicin IC50 percent by half, Activity=2.6μM	19725578
2008/MRP1	Function assay			Inhibition of MRP1 in human 2008/MRP1 cells by Lineweaver-Burke plot analysis, Ki=13.2μM	19725578
2008/MRP1	Function assay			Inhibition of MRP1 in human 2008/MRP1 cells by dixon plot analysis, Ki=13.4μM	19725578
K562	Function assay			Inhibition of P-glycoprotein-mediated multidrug resistance in human doxorubicin-resistant K562 cells assessed as drug level causing 50% increase in nuclear concentration of pirarubicin by spectrofluorimetry, INH=1.6μM	20104851
K562	Function assay			Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for maximum increase in nuclear concentration of pirarubicin by fluorescence assay, Alpha max=0.7μM	21145739
K562	Function assay			Inhibition of Pgp-mediated multidrug resistance in doxorubicin-resistant human K562 cells assessed as drug level required for 50% increase in nuclear concentration of pirarubicin by fluorescence assay, IC50=1.6μM	21145739
HEK-293	Function assay			Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA, IC50=41.5μM	21300721
HCT15	Function assay			Inhibition of ABC transporter in human HCT15 cells assessed as calcein-AM efflux up to 100 uM	21348461
HCT15	Cytotoxicity assay			Cytotoxicity against MDR1 expressing human HCT15 cells	21348461
A2780adr	Function assay			Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay, IC50=5.4μM	21354800
MDCK	Function assay			Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry, IC50=9.8μM	21354800
MDA435/LCC6MDR	Function assay			Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Lineweaver-Burk plot analysis, Ki=1.75μM	22320402
MDA435/LCC6MDR	Function assay			Competitive inhibition of P-gp overexpressed in human MDA435/LCC6MDR cells assessed as accumulation of doxorubicin by Dixon plot analysis, Ki=1.75μM	22320402
HEK293	Function assay			Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=32μM	22587986
BHK	Function assay			Binding affinity to human His10-tagged P-gp expressed in BHK cells assessed as induction of ATPase activity measured as inorganic phosphate release by spectrophotometric analysis, Km=24μM	22727780
ovary cells	Function assay			Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in Chinese hamster ovary cells heterologically expressing alpha-1C subunit, IC50=23.5μM	22761000
embryonic kidney cells	Function assay			Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit, IC50=24μM	22761000
embryonic kidney cells	Function assay			Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit, IC50=47μM	22761000
L929	Function assay			Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method, IC50=8μM	23084278
K562	Function assay			Inhibition of P-glycoprotein in human doxorubicin-resistant K562 cells assessed as half maximal increase of pirarubicin accumulation by spectrofluorometric analysis, IC50=1.6μM	23245571
CHO	Function assay			Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits, IC50=0.2μM	23812503
MDA435/LCC6MDR	Function assay			Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50=0.4457μM	24171478
K562/DOX	Function assay			Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay, IC50=1.6μM	25282263
MDA435/LCC6MDR	Function assay			Modulation of P-gp in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50=0.446μM	26233798
NIH/3T3	Cytotoxicity assay			Intrinsic cytotoxicity against mouse NIH/3T3 cells by MTT assay, CC50=27μM	26836364
CHO	Function assay			Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method, IC50=0.53μM	28797771
K562/Dox	Function assay			Inhibition of P-gp in human K562/Dox cells assessed as increase in nuclear accumulation of pirarubicin by spectrofluorometric assay, IC50=1.6μM	29162309
K562/Dox	Function assay			Inhibition of P-gp in human K562/Dox cells assessed as compound concentration causing 50% increase in nuclear accumulation of pirarubicin by spectrofluorometric method, Activity=1.6μM	29421572
12D7-MDR	Function assay			Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate, IC50=1.2μM	31505928
CHO	Cytotoxicity assay			Cytotoxicity against CHO cells by MTT assay, IC50=0.56μM	ChEMBL
CHRC5	Function assay			Tested for in vitro proliferation and viability of multidrug resistant CHRC5 Chinese hamster cells in the presence and absence of doxorubicin in a modified MTT assay, EC50=1.2μM	ChEMBL
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生物活性

製品説明

Targets

Calcium channel ^[2]

In Vitro
In vitro	The enzyme hydrolase activity of recombinant CES2 is substantially inhibited by diltiazem and verapamil (Ki = 0.25 ± 0.02 and 3.84 ± 0.99μM, respectively).

In Vivo
In Vivo	Verapamil confers an anti-arrhythmic effect via calcium influx inhibition, inhibition of oxygen consumption and accompanied by preservation of Cx43 protein in rat heart.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05618132	Recruiting	Angina Pectoris Variant\|Angina Pectoris; Spasm-Induced\|Angina Pectoris With Normal Coronary Arteriogram	University Hospital Antwerp	January 9 2023	Not Applicable
NCT04406259	Recruiting	Cluster Headache	Centre Hospitalier Universitaire de Nice	November 2 2020	Phase 4
NCT04014634	Completed	Cluster Headache Episodic\|Greater Occipital Nerve Injection	Leiden University Medical Center\|Netherlands Brain Foundation\|Innovatiefonds Zorgverzekeraars	August 1 2019	Phase 4

参考
[1] Yanjiao X, et al. Drug Metab Pharmacokinet, 2013. [2] Zhou P, et al. PLoS One, 2013, 8(8), e71567. [3] Gowarty JL, et al. J Oncol Pharm Pract. 2019 Apr;25(3):743-746.

参考

化学情報

分子量	491.06	化学式	C₂₇H₃₈N₂O₄.HCl
CAS No.	152-11-4	SDF	Download Verapamil HCl SDFをダウンロードする
Smiles	CC(C)C(CCCN(C)CCC1=CC(=C(C=C1)OC)OC)(C#N)C2=CC(=C(C=C2)OC)OC.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 98 mg/mL ( (199.56 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 98 mg/mL

Ethanol : 98 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):