Nelfinavir Mesylate

別名：AG 1343 Mesylate

製品コード：S4282 純度：99.51%

Nelfinavir Mesylate is a potent HIV protease inhibitor with K_i of 2 nM.

CAS No. 159989-65-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 61300	国内在庫あり

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（17）

製品安全説明書

現在のバッチを見る：純度： 99.51%

99.51

Nelfinavir Mesylate関連製品

関連ターゲット	HIV-1 capsid HIV-1 caspid	もっと見る
関連製品	Pepstatin A Limonin Temsavir (BMS-626529)	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	もっと見る

シグナル伝達経路

HIV Proteaseシグナル伝達経路

HIV Protease阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
12D7	Antiviral assay	0.08 to 1.25 uM	3 days	Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 0.08 to 1.25 uM incubated for 3 days followed by replacement of fresh medium containing compound and measured after 3 days by ELISA	31505928
HEK293	Function assay	0.12 uM		Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as unprocessed gp160 Env protein at 0.12 uM by Western blot	17646410
HEK293	Function assay	0.12 uM		Inhibition of HIV1 NL4-3 proteins incorporation into virions transfected in HEK293 cells assessed as aberrant Env protein at 0.12 uM by Western blot	17646410
MDR1	Function assay	20 uM		Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM	17664327
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E, EC50=0.011μM.	18955518
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA, EC50=0.17μM.	18955518
MT4	Antiviral assay	1 uM		Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA, EC50=0.21μM.	18955518
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA, EC50=0.24μM.	18955518
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA, EC50=0.32μM.	18955518
MT4	Antiviral assay	1 uM		Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA, EC50=0.51μM.	18955518
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA, EC50=0.65μM.	18955518
MT4	Antiviral assay	1 uM		Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay, EC50=0.22μM.	20439612
MT4	Antiviral assay	1 uM		Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay, EC50=0.29μM.	20439612
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay, EC50=0.3μM.	20439612
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay, EC50=0.32μM.	20439612
MT4	Antiviral assay	1 uM		Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay, EC50=0.37μM.	20439612
MT4	Antiviral assay	5 uM		Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay, EC50=0.51μM.	20439612
CEM-SS	Antiviral assay		6 days	Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay, ED50=0.03μM.	15217281
HOG.R5	Antiviral assay		4 days	Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=0.09μM.	15217281
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.018μM.	17576848
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=0.048μM.	17576848
CEM	Antiviral assay		7 days	Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.1μM.	17576848
CEM	Antiviral assay		7 days	Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.177μM.	17576848
CEM	Antiviral assay		7 days	Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.199μM.	17576848
CEM	Antiviral assay		7 days	Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay, EC50=0.281μM.	17576848
HEK293	Antiviral assay		48 hrs	Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay, EC50=0.0058μM.	17638694
MT4	Antiviral assay		6 days	Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay, EC50=0.029μM.	17638694
MT4	Cytotoxicity assay		6 days	Cytotoxicity against human MT4 cells after 6 days by MTT assay, CC50=8μM.	17638694
CEM-SS	Antiviral assay		5 days	Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as reverse transcriptase activity after 5 days by MTT assay, IC50=0.002μM.	17950955
MOLT-4/3B	Antiviral assay		4 days	Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay, EC50=0.029μM.	18316521
MT2	Antiviral assay		7 days	Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay, EC50=0.023μM.	18955518
HeLa	Antiviral assay		72 hrs	Antiviral activity against HIV1 harboring capsid I201V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.013μM.	19805571
HeLa	Antiviral assay		72 hrs	Antiviral activity against wild type HIV1 infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.016μM.	19805571
HeLa	Antiviral assay		72 hrs	Antiviral activity against HIV1 harboring spacer peptide A1V mutant protein infected in human HeLa cells assessed as decrease in viral infection after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.038μM.	19805571
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against wild type HIV1 subtype C infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.00167μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against wild type HIV1 subtype CRF02_AG infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0057μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against wild type HIV1 subtype B infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.0098μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position and M46 mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay, EC50=0.055μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype CRF02_AG harboring protease L33I, M46I, A71T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte, EC50=0.202μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype C harboring protease L23I, M46I, L89T mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene , EC50=0.272μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype B harboring protease D30N, M46I, A71T and V77I mutant gene and polymorphism at M36 position of protease infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luci, EC50=1.139μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype B harboring protease D30N, L33I, M46I, N88D mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=1.463μM.	20404123
cord blood mononuclear cells	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype C harboring protease D30N, E35G, I85V, L90M mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter, EC50=3.473μM.	20404123
TZM-bl	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay	20404123
TZM-bl	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay	20404123
TZM-bl	Antiviral assay		48 hrs	Antiviral activity against HIV1 subtype B harboring protease polymorphism at I36 position infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay	20404123
BESM	Antitrypanosomal assay		88 hrs	Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay, EC50=12μM.	20547819
BESM	Cytotoxicity assay		88 hrs	Cytotoxicity against BESM cells after 88 hrs by HTS assay, EC50=32μM.	20547819
CMEC/D3	Function assay		30 mins	Inhibition of P-gp in human CMEC/D3 cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=1.7μM.	31505928
CMEC/D3	Function assay		30 mins	Inhibition of P-gp in human CMEC/D3 cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=2μM.	31505928
12D7-MDR	Function assay		30 mins	Inhibition of P-gp in human 12D7-MDR cells using NBD-Aba as substrate after 30 mins by flow cytometric analysis, IC50=5.8μM.	31505928
12D7-MDR	Function assay		30 mins	Inhibition of P-gp in human 12D7-MDR cells using calcein-AM as substrate after 30 mins by flow cytometric analysis, IC50=9.1μM.	31505928
12D7	Antiviral assay		3 days	Antiviral activity against HIV1 LAI infected in human 12D7 cells overexpressing p-gp assessed as reduction in P24 level at 1:1 ratio of test compound to abacavir incubated for 3 days followed by followed by replacement of fresh medium containing compound	31505928
MT2	Antiviral assay		5 days	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.0049μM.	ChEMBL
HepG2	Cytotoxicity assay		5 days	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=7.4μM.	ChEMBL
skeletal myoblast cells	Cytotoxicity assay		72 hours	DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50=12.05μM.	ChEMBL
MT2	Cytotoxicity assay		5 days	Cytotoxicity against human MT2 cells assessed as reduction in cell viability after 5 days by XTT assay, CC50=19.1μM.	ChEMBL
HeLa	Function assay			TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in OCT1-expressing HeLa cells, IC50=21.8μM.	10681378
Caco-2	Function assay			TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 5 uM) in Caco-2 cells, IC50=1.4μM.	10820137
MT-4	Antiviral assay			Anti-HIV-1 activity against Wild type virus in MT-4 cells, ED50=0.02μM.	11543677
MT-4	Antiviral assay			Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with compound 1), ED50=0.07μM.	11543677
MT-4	Antiviral assay			Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with ritonavir), ED50=0.11μM.	11543677
MT-4	Antiviral assay			Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with saquinavir), ED50=0.12μM.	11543677
MT-4	Antiviral assay			Anti-HIV-1 activity against mutant HIV-1 in MT-4 cells (mutation selected with nelfinavir), ED50=2.44μM.	11543677
LLC-PK1	Function assay			Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=2.3μM.	12699389
LLC-PK1	Function assay			TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells, IC50=2.3μM.	12699389
LLC-PK1	Function assay			Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=3.4μM.	12699389
LLC-PK1	Function assay			TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells, IC50=3.4μM.	12699389
HEK	Function assay			TP_TRANSPORTER: increase in mitoxantrone intracellular accumulation in BCRP-expressing HEK cells, IC50=12.5μM.	15007102
MT-4	Function assay			Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells, ED50=0.02μM.	15537350
MT4	Antiviral assay			Antiviral activity against HIV1 HXB2 in MT4 cells, IC50=0.32μM.	16458505
MT4	Antiviral assay			Antiviral activity against HIV1 EP13 in MT4 cells, IC50=0.45μM.	16458505
PHA-PBMC	Antiviral assay			Antiviral activity against HIV1 BA-L isolate in human PHA-PBMC cells, IC50=0.007μM.	16913714
MT2	Antiviral assay			Antiviral activity against HIV1 LAI isolate in human MT2 cells, IC50=0.01μM.	16913714
PHA-PBMC	Antiviral assay			Antiviral activity against HIV1 LAI isolate in human PHA-PBMC cells, IC50=0.014μM.	16913714
MT2	Antiviral assay			Antiviral activity against HIV2 EHO isolate in human MT2 cells, IC50=0.02μM.	16913714
PHA-PBMC	Antiviral assay			Antiviral activity against multi drug-resistant HIV1 ET variant in human PHA-PBMC cells, IC50=0.032μM.	16913714
PHA-PBMC	Antiviral assay			Antiviral activity against multi drug-resistant HIV1 G variant in human PHA-PBMC cells, IC50=0.17μM.	16913714
PHA-PBMC	Antiviral assay			Antiviral activity against multi drug-resistant HIV1 C variant in human PHA-PBMC cells, IC50=0.31μM.	16913714
MT2	Antiviral assay			Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.03μM.	17371811
MT2	Antiviral assay			Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.032μM.	17371811
MT4	Antiviral assay			Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay, EC50=0.033μM.	17371811
MT4	Antiviral assay			Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.08μM.	17371811
MT4	Antiviral assay			Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.21μM.	17371811
MT4	Antiviral assay			Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.22μM.	17371811
MT2	Antiviral assay			Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.24μM.	17371811
MT4	Antiviral assay			Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM.	17371811
MT4	Antiviral assay			Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.27μM.	17371811
MT4	Antiviral assay			Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.34μM.	17371811
MT4	Antiviral assay			Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.47μM.	17371811
MT4	Antiviral assay			Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.48μM.	17371811
MT4	Antiviral assay			Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay, EC50=0.49μM.	17371811
MT2	Cytotoxicity assay			Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay, CC50=8.1μM.	17371811
MT4	Antiviral assay			Antiviral activity against HIV1 3B in MT4 cells by MTT assay, EC50=0.016μM.	17537628
MT4	Cytotoxicity assay			Cytotoxicity against MT4 cells by MTT assay, LC50=11μM.	17537628
MDCK2	Inhibition of human			Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50=19.9μM.	17664327
MT4	Antiviral assay			Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced cytopathic effect by MTT method, EC50=0.016μM.	18426195
MT4	Cytotoxicity assay			Cytotoxicity against human MT4 cells by MTT assay, CC50=11μM.	18426195
MT4	Antiretroviral assay			Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.023μM.	18541726
MT4	Antiretroviral assay			Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.028μM.	18541726
MT4	Antiviral assay			Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.029μM.	18541726
MT4	Antiviral assay			Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.035μM.	18541726
MT4	Antiretroviral assay			Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.049μM.	18541726
MT4	Antiretroviral assay			Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM.	18541726
MT4	Antiretroviral assay			Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.05μM.	18541726
MT4	Antiviral assay			Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay, EC50=0.17μM.	18541726
MT4	Antiviral assay			Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA, EC50=0.018μM.	18955518
MT4	Antiviral assay			Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay, EC50=0.045μM.	20439612
MT4	Antiviral assay			Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay, EC50=0.13μM.	20439612
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
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生物活性

製品説明

Nelfinavir Mesylate is a potent HIV protease inhibitor with K_i of 2 nM.

Targets

HIV protease ^[1]
(Cell-free assay)

2 nM(Ki)

In Vivo
In Vivo	In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. Initial investigation of the compound in fed rats indicated an oral bioavailability of 43%. In contrast, the oral bioavailability was significantly reduced in fasted rats to 29%. Nelfinavir demonstrated significant oral bioavailabilability across a range of species including dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). It has a long plasma half-life after oral dosing that is likely due to a combination of slow dissolution and absorption. nelfinavir is well absorbed in humans particularly when administered with food and possesses minimal and easily managed side effects^[1].
動物実験	動物モデル	Sprague-Dawley rats
	投与量	12.5 to 25 mg/kg (i.v); 25 to 50 mg/kg (oral)
	投与経路	i.v and oral administration

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00051844	Completed	Human Immunodeficiency Virus	Pfizer	August 2002	Phase 2

参考
[1] Kaldor SW, et al.J Med Chem, 1997,40(24):3979-85.

参考

[1] Kaldor SW, et al.J Med Chem, 1997,40(24):3979-85.

化学情報

分子量	663.89	化学式	C₃₃H₄₉N₃O₇S₂
CAS No.	159989-65-8	SDF	Download Nelfinavir Mesylate SDFをダウンロードする
Smiles	CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O.CS(=O)(=O)O
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 : 100 mg/mL ( (150.62 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。)

Ethanol : 100 mg/mL

Water : Insoluble

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。

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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):