Lamivudine

別名：GR109714X, BCH-189

製品コード：S1706 純度：99.94%

Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase.

CAS No. 134678-17-4

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
25mg	JPY 37000	国内在庫あり
50mg	JPY 52000	国内在庫あり
1g	JPY 145500	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1例

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

Lamivudine関連製品

関連ターゲット	HBV RT HIV RT RT	もっと見る
関連製品	Dapivirine (TMC120) Salicylanilide Fangchinoline	もっと見る
関連化合物ライブラリー	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	もっと見る

シグナル伝達経路

Reverse Transcriptaseシグナル伝達経路

Reverse Transcriptase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
PBMC	Function assay	300 mg	7 days	Cmax in HIV-infected human assessed as Lamivudine monophosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000008μM	17664328
PBMC	Function assay	300 mg	7 days	Cmax in HIV-infected human assessed as Lamivudine diphosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000044μM	17664328
PBMC	Function assay	300 mg	7 days	Cmax in HIV-infected human assessed as Lamivudine triphosphate level in PBMC at 300 mg QD for 7 days measured per 10'6 cells in presence of zidovudine, Cmax=0.0000048μM	17664328
HepG2(2.2.15)	Antiviral assay	13 uM	72 hrs	Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA level at 13 uM after 72 hrs by RT-PCR analysis	20176893
HepG2(2.2.15)	Function assay	0.75 to 3 uM	72 hrs	Decrease in HBV viral DNA replication in human HepG2(2.2.15) cells at 0.75 to 3 uM after 72 hrs by real-time PCR analysis, IC50=7.63μM	25461891
U87	Antiviral assay	10 uM	4 days	Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 10 uM measured after 4 days by p24 ELISA	27091070
U87	Antiviral assay	100 uM	4 days	Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 100 uM measured after 4 days by p24 ELISA	27091070
HepG2.2.15	Function assay	4 uM	6 days	Inhibition of capsid protein in Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction in viral DNA level at 4 uM supplemented with fresh medium containing compound every 2 days and measured after 6 days by RT-PCR analysis, IC50<0.1μM	31091479
MDCK2	Function assay	10 uM		Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay	17172311
MDCK2	Function assay	10 uM		Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay	17172311
MDCK2	Function assay	10 uM		Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay	17172311
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=0.36μM	15217281
HOG.R5	Antiviral assay		4 days	Antiviral activity against HIV1 3B infected in human HOG.R5 cells after 4 days, IC50=1.2μM	15217281
Huh7	Antiviral assay		5 days	Antiviral activity against HBV genotype D with reverse transcriptase L80I mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.03μM	17438047
Huh7	Antiviral assay		5 days	Antiviral activity against HBeAg-deficient HBV genotype D with precore G1896A mutation and reverse transcriptase L80I mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.03μM	17438047
Huh7	Antiviral assay		5 days	Antiviral activity against HBV genotype D in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.41μM	17438047
Huh7	Antiviral assay		5 days	Antiviral activity against HBeAg-deficient HBV genotype D with precore G1896A mutation in human Huh7 cells assessed as inhibition of viral replication after 5 days, EC50=0.46μM	17438047
HepG2.2.15	Function assay		8 days	Inhibition of cytoplasmic HBV DNA synthesis in HepG2.2.15 cells after 8 days, IC50=0.38μM	17499889
MAGIC-5A	Antiviral assay		40 hrs	Antiviral activity against wild type HIV1 NL4-3 produced from full length pR9deltaApa infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=0.88μM	17967913
MAGIC-5A	Antiviral assay		40 hrs	Antiviral activity against wild type HIV2 ROD produced from full length pROD9 infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=2μM	17967913
MAGIC-5A	Antiviral assay		40 hrs	Antiviral activity against multinucleoside-resistant HIV1 NL4-3 harboring A62V, V75I, F77L, F116Y, Q151M mutation in viral reverse transcriptase infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs, EC50=3.7μM	17967913
PBMC	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.04μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.04μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.063μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.086μM	18316521
MT2	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.105μM	18316521
MT2	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.171μM	18316521
MT2	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.182μM	18316521
MT2	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.183μM	18316521
MT2	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.202μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.219μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA, EC50=0.372μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=0.462μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.554μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=0.667μM	18316521
PBMC	Antiviral assay		1 hr	Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.85μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.927μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay, EC50=0.969μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay, EC50=1.14μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=1.259μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=1.683μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=1.985μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=2.445μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA, EC50=2.47μM	18316521
MT2	Antiviral assay		5 days	Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay, EC50=3.247μM	18316521
HepG2(2.2.15)	Antiviral assay		24 hrs	Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as extracellular HBV virion DNA level after 24 hrs, EC50=0.048μM	19072694
HepG2(2.2.15)	Antiviral assay		24 hrs	Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as replication intermediates after 24 hrs, EC50=0.15μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against lamivudine-resistant wild type HBV in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=0.2μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against lamivudine-resistant HBV reverse transcriptase 236T mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=0.3μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against adefovir-resistant wild type HBV in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.3μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against adefovir-resistant HBV reverse transcriptase M204V mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.5μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against adefovir-resistant HBV reverse transcriptase L180M mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.6μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against adefovir-resistant HBV reverse transcriptase LM/reverse transcriptase MV double mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.6μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against adefovir-resistant HBV reverse transcriptase M204I mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=1.8μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against adefovir-resistant HBV reverse transcriptase 236T mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=7.7μM	19072694
Huh7	Antiviral assay		4 days	Antiviral activity against lamivudine-resistant HBV reverse transcriptase L180M mutant in human Huh7 cells after 4 days by intracellular HBV DNA replication assay, EC50=10μM	19072694
HuH7	Antiviral assay		24 hrs	Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=0.2μM	19398648
HuH7	Antiviral assay		24 hrs	Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=0.3μM	19398648
HuH7	Antiviral assay		24 hrs	Antiviral activity against HBV harboring RNA polymerase N236T mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=1.5μM	19398648
HuH7	Antiviral assay		24 hrs	Antiviral activity against wild type HBV infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=3μM	19398648
HuH7	Antiviral assay		24 hrs	Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC50=16μM	19398648
HuH7	Antiviral assay		24 hrs	Antiviral activity against HBV harboring RNA polymerase L180M mutant gene infected in human HuH7 cells assessed as decrease in viral transient transfection after 24 hrs, EC90=41μM	19398648
TZM-bl	Antiviral assay		72 hrs	Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=0.47μM	19704131
TZM-bl	Antiviral assay		72 hrs	Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=1.08μM	19704131
TZM-bl	Antiviral assay		72 hrs	Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S/T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay, EC50=2.1μM	19704131
1.3ES2	Antiviral assay		6 days	Antiviral activity against Hepatitis B virus ayw in human 1.3ES2 cells stably transfected with 1.3 fold wild type HBV ayw strain genome cells assessed as reduction of viral DNA level after 6 days by RT-PCR	20061158
HepG2.2.15	Antiviral assay		9 days	Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=0.2μM	20117930
HepG2.2.15	Antiviral assay		9 days	Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=0.2μM	20117930
HepG2.2.15	Antiviral assay		9 days	Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=0.7μM	20117930
HepG2.2.15	Antiviral assay		9 days	Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=0.8μM	20117930
HepG2.2.15	Antiviral assay		9 days	Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC50=5.3μM	20117930
HepG2.2.15	Antiviral assay		9 days	Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization, EC90=20μM	20117930
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype D isolate 8 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.25μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype A isolate 1 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.54μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype C isolate 6 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=3.9μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype C isolate 7 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.06μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype BF isolate 5 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.24μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype A isolate 2 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.48μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 NL4-3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.68μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype B isolate 3 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=4.78μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 subtype B isolate 4 infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=5.43μM	20308377
HEK293	Antiviral assay		72 hrs	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C/G190A mutant infected in HEK293 cells assessed as inhibition of virus replication after 72 hrs, EC50=7.16μM	20308377
HepG2(2.2.15)	Antiviral assay		8 days	Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral cytoplasmic DNA synthesis after 8 days by RT-PCR analysis, IC50=0.16μM	20639110
HepG2(2.2.15)	Cytotoxicity assay		8 days	Cytotoxicity against human HepG2(2.2.15) cells after 8 days by MTT assay, CC50=5μM	20639110
MT2	Antiviral assay		2 to 3 days	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR, EC50=0.8μM	21115794
Huh7	Antiviral assay		1 day	Antiviral activity against Hepatitis B virus infected in human Huh7 cells assessed as reduction in viral DNA after 1 day by Southern blotting, EC50=0.1μM	21333535
HuH7	Cytotoxicity assay		4 days	Cytotoxicity against human HuH7 cells after 4 days by neutral red dye uptake assay, CC50=0.1μM	21333535
HepG2(2.2.15)	Antiviral assay		4 days	Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 4 days by RT-PCR analysis, IC50=0.33μM	21524588
HepG2(2.2.15)	Antiviral assay		9 days	Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization method, EC50=0.2μM	21930377
HepG2(2.2.15)	Antiviral assay		9 days	Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization meth, EC50=0.2μM	21930377
HepG2(2.2.15)	Antiviral assay		9 days	Antiviral activity against wild type Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybridization assay, EC90=0.6μM	21930377
HepG2(2.2.15)	Antiviral assay		9 days	Antiviral activity against adefovir-resistant Hepatitis B virus harboring reverse transcriptase N236T mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hybri, EC90=0.9μM	21930377
HepG2(2.2.15)	Antiviral assay		9 days	Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as inhibition of virus replication treated daily for 9 days by quantitative blot hybridization me, EC50=1.5μM	21930377
HepG2(2.2.15)	Antiviral assay		9 days	Antiviral activity against lamivudine-resistant Hepatitis B virus harboring reverse transcriptase L180M mutant infected in human HepG2(2.2.15) cells assessed as reduction of infectious virus titer treated daily for 9 days by quantitative Southern blot hyb, EC90=22μM	21930377
HeLa P4/R5	Antiviral assay		2 hrs	Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay, EC50=11.3μM	22352809
HeLa P4/R5	Antiviral assay		2 hrs	Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay, EC50=32.7μM	22352809
HeLa P4/R5	Antiviral assay		2 hrs	Antiviral activity against HIV1 BaL assessed as inhibition of infection in HeLa P4/R5 cells expressing CD4 receptor and beta-gal incubated for 2 hrs followed by compound-wash out measured after 46 hrs by single round infection MAGI assay, EC50=11.4μM	22533850
HeLa P4/R5	Antiviral assay		2 hrs	Antiviral activity against HIV1 3B assessed as inhibition of infection in HeLa P4/R5 cells expressing CD4 receptor and beta-gal incubated for 2 hrs followed by compound-wash out measured after 46 hrs by single round infection MAGI assay, EC50=32.7μM	22533850
CEM-SS	Antiviral assay		6 days	Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay, EC50=0.2μM	22858097
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay, EC50=1.8μM	24119448
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay, EC50=5.9μM	24119448
CEM	Antiviral assay		4 days	Antiviral activity against HIV1 3B infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis, EC50=0.099μM	24177359
CEM	Antiviral assay		4 days	Antiviral activity against HIV2 ROD infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis, EC50=0.18μM	24177359
MT4	Antiviral assay		5 days	Antiviral activity against Human immunodeficiency virus 1 3b infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay, IC50=3.9μM	24926807
MT4	Antiviral assay		5 days	Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay, IC50=15.5μM	24926807
MT4	Antiviral assay		5 days	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, IC50=3.89μM	24952305
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay, IC50=15.53μM	24952305
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay, EC50=2.22μM	25240095
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay, EC50=8.81μM	25240095
MT4	Antiviral assay		5 days	Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.24μM	25537532
MT4	Antiviral assay		5 days	Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay, EC50=8.79μM	25537532
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.239μM	25626145
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay, EC50=0.89μM	25682562
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay, EC50=3.56μM	25682562
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.2μM	25707013
MT4	Antiviral assay		5 days	Antiviral activity against HIV1-3B infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay, EC50=3.9μM	25946116
MT4	Antiviral assay		5 days	Antiviral activity against HIV2-ROD infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay, EC50=15.5μM	25946116
HepG22.2.15	Antiviral assay		3 days	Antiviral activity against HBV infected in human HepG22.2.15 cells after 3 days by neutral red dye-based plaque reduction assay, IC50=0.039μM	26260336
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=3.1μM	27267005
HepG2.2.15.7	Antiviral assay		9 days	Antiviral activity against HBV infected in human HepG2.2.15.7 cells assessed as inhibition of viral DNA level after 9 days by real time PCR method, EC50=0.03μM	27426303
MT4	Antiviral assay		5 days	Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay, EC50=2.24μM	27541578
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay, EC50=8.79μM	27541578
HepG2(2.2.15)	Antiviral assay		6 days	Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days by real-time qPCR method, EC50<0.01μM	27748590
HepG2(2.2.15)	Antiviral assay		6 days	Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method, EC50=0.01μM	27748590
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.22μM	27748590
MT4	Antiviral assay		5 days	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay, EC50=8.81μM	27748590
HepAD38	Antiviral assay		5 days	Antiviral activity against HBV infected in human HepAD38 cells assessed as inhibition of DNA replication after 5 days by RT-PCR method, EC50=0.04μM	28094179
P4R5 MAGI	Function assay		2 hrs	Inhibition of HIV1 BaL dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay, EC50=11.3μM	28351588
P4R5 MAGI	Function assay		2 hrs	Inhibition of HIV1 3B dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay, EC50=32.7μM	28351588
HepG2.2.15	Antiviral assay		8 days	Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of viral DNA replication after 8 days by real time fluorescent PCR method, IC50=0.5μM	28494252
MT4	Antiviral assay		5 days	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=2.54μM	28659246
HepG2(2.2.15)	Antiviral assay		6 days	Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring intracellular viral DNA copy number after 6 days byr by real-time qPCR assay, EC50=0.00887μM	28682067
HepG2(2.2.15)	Antiviral assay		6 days	Antiviral activity against HBV ayw1 infected in human HepG2(2.2.15) cells assessed as reduction in viral replication by measuring extracellular viral DNA copy number after 6 days by real-time qPCR method, EC50=0.02μM	28682067
SupT1	Antiviral assay		48 hrs	Antiviral activity against VSV-G pseudotyped HIV1 infected in human SupT1 cells after 48 hrs by luciferase reporter gene assay, IC50=0.1μM	29016131
HepG2(2.2.15)	Antiviral assay		6 days	Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as inhibition of viral DNA replication after 6 days by RT-PCR method, IC50<0.1μM	29288943
HepG2.2.15	Antiviral assay		6 days	Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as reduction in extracellular viral DNA levels after 6 days by qPCR/TaqMan assay, IC50=0.025μM	30286292
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 RES056 containing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=7.77μM	30606670
MT4	Antiviral assay		5 days	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay, EC50=12.8μM	30606670
MT4	Antiviral assay		5 days	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay, EC50=6.41μM	30721060
C8166	Antiviral assay		72 hrs	Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of syncytial cell formation incubated for 72 hrs, EC50=0.3μM	31310115
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=1.92μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.14μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.58μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.7μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=3.88μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=4.45μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=4.54μM	31434039
MT4	Antiviral assay		5 days	Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay, EC50=5.54μM	31434039
2.2.15	Function assay			In vitro effective concentration against hepatitis B virus was determined in 2.2.15 cells, EC50=0.008μM	9301659
PBMC	Anti-HIV-1 assay			Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=10.1μM	8423591
PBMC	Anti-HIV-1 assay			Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.21μM	8423591
PBMC	Anti-HIV-1 assay			Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.06μM	8423591
PBMC	Anti-HIV-1 assay			Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV, EC50=0.0018μM	8423591
PBMC	Function assay			Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV, EC50=0.21μM	8410975
PBMC	Function assay			Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV, EC50=0.0018μM	8410975
MT-4	Function assay			Concentration required to inhibit syntica formation by 50% in HIV-1 infected MT-4 cells, IC50=0.1μM	8035429
PBMC	Anti-HIV-1 assay			In vitro anti-HIV activity in peripheral blood mononuclear cells, EC50=0.07μM	9301659
2.2.15	Antiviral assay			Antiviral activity against Hepatitis B virus (HBV) in 2.2.15 cells, EC50=0.008μM	11052795
PBMC	Antiviral assay			Antiviral activity against Immunodeficiency virus type-1 (HIV-1) in peripheral blood mononuclear cells, EC50=0.07μM	11052795
H9	Antiviral assay			Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique, EC50=0.06μM	11430019
H9	Antiviral assay			Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique, EC50=0.06μM	11430019
PBMC	Antiviral assay			Antiviral activity against HIV-1xxBRU mutant strain in human PBM cells, EC90=0.08μM	12383014
PBMC	Function assay			Activity against Lamivudine-resistant virus (HIV-1XXBRU) in human PBM cells, expressed as EC50, EC50=0.035μM	12852755
PBMC	Function assay			In vitro concentration required to inhibit the HIV-1 LA1 replication on PBMCs cell (peripheral blood mononuclear cells), EC50=0.01μM	12852943
PBMC	Function assay			Effective concentration to inhibit HIV-1 LAI cytopathicity in PBMC cells was determined in vitro, EC50=0.0116μM	14971898
HepG2.2.15	Function assay			Effective concentration to inhibit hepatitis B virus cytopathicity in HepG2.2.15 cells was determined in vitro, EC50=0.2μM	14971898
MT-4	Function assay			Effective concentration to inhibit HIV-1 IIIB cytopathicity in MT-4 cells was determined in vitro, EC50=0.5μM	14971898
PBMC	Antiviral assay			Antiviral activity against wild type HIV virus(xxBRU) in Human peripheral blood mononuclear (PBM) cells, EC90=0.08μM	15027854
PBMC	Function assay			Effective concentration against Wild Type HIV-1 virus in human peripheral blood mononuclear cells, EC50=0.041μM	15189036
2.2.15	Function assay			Inhibition of HBV replication in 2.2.15 cells by DNA hybridization assay, EC50=0.02μM	15615545
2.2.15	Function assay			Effective concentration required to inhibit hepatitis B virus replication in 2.2.15 cells in DNA hybridization assay, EC50=0.05μM	15634003
PBMC	Function assay			In vitro effective concentration against Lamivudine resistant wild type HIV-1 in human peripheral blood mononuclear cells, EC50=0.027μM	15916425
PBMC	Function assay			In vitro effective concentration against Lamivudine resistant wild type HIV-1 in human peripheral blood mononuclear cells, EC90=0.25μM	15916425
2.2.15	Function assay			Effective concentrations at which 2-fold depression of extracellular virion DNA (HBV) was observed in 2.2.15 Cells, EC50=0.06μM	16033283
2.2.15	Function assay			Effective concentrations at which 2-fold depression of extracellular virion DNA (HBV) was observed in 2.2.15 Cells, EC90=0.17μM	16033283
2.2.15	Function assay			Effective concentrations at which 10-fold depression of intracellular intermediates of HBV DNA was observed in 2.2.15 Cells, EC50=0.23μM	16033283
2.2.15	Function assay			Effective concentrations at which 10-fold depression of intracellular intermediates of HBV DNA was observed in 2.2.15 Cells, EC90=0.69μM	16033283
2.2.15	Function assay			Inhibition of synthesis of extracellular virion DNA release in cultured human hepatoblastoma 2.2.15 cells, EC50=0.048μM	16213713
2.2.15	Function assay			Inhibition of synthesis of extracellular virion DNA release in cultured human hepatoblastoma 2.2.15 cells, EC90=0.151μM	16213713
2.2.15	Function assay			Inhibition of synthesis of intracellular HBV DNA replicative intermediates in cultured human hepatoblastoma 2.2.15 cells, EC50=0.251μM	16213713
2.2.15	Function assay			Inhibition of synthesis of intracellular HBV DNA replicative intermediates in cultured human hepatoblastoma 2.2.15 cells, EC90=0.648μM	16213713
2.2.15	Function assay			Inhibition of wild type HBV transfected in human hepatoblastoma 2.2.15 cells, EC50=2.1μM	16539393
hepatoma 2.2.15	Antiviral assay			Antiviral activity against wild type HBV in human hepatoma 2.2.15 cells, EC50=2.1μM	16759112
2.2.15	Function assay			Inhibition of HBV replication in 2.2.15 cells by DNA hybridization assay, EC50=0.02μM	17004726
Huh7	Function assay			Inhibition of wild type HBV replication in Huh7 cells, EC50=1μM	17371827
PBMC	Antiviral assay			Antiviral activity against HIV1 LAI in human PBM cells, EC50=0.026μM	17403996
PBMC	Antiviral assay			Antiviral activity against HIV1 LAI in human PBM cells, EC90=0.12μM	17403996
HepG2.2.15	Antiviral assay			Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR, EC50=0.1μM	17404006
HepG2(2.2.15)	Antiviral assay			Antiviral activity against HBV in ayw wild type HepG2(2.2.15) cells assessed as inhibition of viral DNA replication, IC50=0.05μM	17488817
HepG2(2.2.15)	Function assay			Inhibition of HBV promoter in human HepG2(2.2.15) cells by luciferase reporter gene assay, IC50=0.08μM	17488817
HepW10	Antiviral assay			Antiviral activity against HBV in adriamycin-resistant wild type HepW10 cells assessed as inhibition of viral DNA replication, IC50=0.1μM	17488817
HBV-Met	Antiviral assay			Antiviral activity against HBV in mouse ayw wild type HBV-Met cells assessed as inhibition of viral DNA replication, IC50=0.2μM	17488817
MT2	Antiviral assay			Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells, EC50=0.04μM	18316521
MT2	Antiviral assay			Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA, EC50=0.047μM	18316521
PBMC	Antiviral assay			Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.071μM	18316521
PBMC	Antiviral assay			Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA, EC50=0.081μM	18316521
MT2	Antiviral assay			Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.6μM	19596885
HeLa P4/R5	Antiviral assay			Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=0.78μM	19596885
TZM-bl	Antiviral assay			Antiviral activity against wild-type HIV1 pNL4-3 infected in TZM-bl cells by luciferase assay, EC50=0.65μM	19704131
HepG2.2.15	Antiviral assay			Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA replication, IC50=0.22μM	19897363
MT2	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V, M184I mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysis, EC50=0.8μM	21115794
MT2	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysis, EC50=0.8μM	21115794
MT2	Antiviral assay			Antiviral activity against Human immunodeficiency virus 1 3B harboring reverse transcriptase M184V, M184I, K82N mutant infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected on day 14 after 4 passages by PCR analysi, EC50=0.8μM	21115794
HepG2(2.2.15)	Antiviral assay			Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in viral DNA by Southern blotting, EC50=0.06μM	21333535
HuH7	Antiviral assay			Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells, EC50=0.056μM	23237841
HuH7	Antiviral assay			Antiviral activity against wild type Hepatitis B virus infected in human HuH7 cells, EC90=0.142μM	23237841
HOG.R5	Antiviral assay			Antiviral activity against HIV-1 3B/H9 infected in human HOG.R5 cells transfected with HIV1 LTR-GFP assessed as inhibition of viral replication by fluorescence analysis, IC50=1.2μM	24404757
MT4	Antiviral assay			Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay, EC50=2.442μM	24794751
MT4	Antiviral assay			Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay, EC50=7.2μM	24794751
HepG2.2.15	Antiviral assay			Antiviral activity against hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of viral replication, IC50=14.17μM	25127104
HepG2.2.15	Antiviral assay			Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as inhibition of HBV DNA replication by real-time fluorescence quantitative PCR analysis, IC50=6.86μM	25847765
Huh7	Antiviral assay			Antiviral activity against lamivudine-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in secreted DNA levels measured on day 7 by real-time PCR analysis, EC50=0.055μM	28082068
HepG2.215	Antiviral assay			Antiviral activity against hepatitis B virus infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis, EC50=0.1μM	28082068
Huh7	Antiviral assay			Antiviral activity against lamivudine-resistant wild type hepatitis B virus infected in human Huh7 cells assessed as reduction in intracellular DNA levels measured on day 7 by real-time PCR analysis, EC50=0.237μM	28082068
HepG2.215	Antiviral assay			Antiviral activity against hepatitis B virus infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis, EC90=2μM	28082068
HepAD38	Antiviral assay			Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method, EC50<0.01μM	28688280
HepAD38	Antiviral assay			Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral replication by RT-PCR method, EC50=0.04μM	28688280
HepAD38	Antiviral assay			Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method, EC50=0.04μM	28688280
HepAD38	Antiviral assay			Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in viral replication by RT-PCR method, EC90=0.3μM	28688280
HepAD38	Antiviral assay			Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in extracellular viral DNA level by RT-PCR method, EC90=0.3μM	28688280
HepAD38	Antiviral assay			Antiviral activity against HBV infected in human HepAD38 cells assessed as reduction in intracellular viral DNA level by RT-PCR method, EC90=0.7μM	28688280
A549	Antiviral assay			Antiviral activity against HIV1 virions derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-mixed virions followed by incubation with target cel, IC50=0.51μM	29699924
HepG2.2.15	Antiviral assay			Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=2.22μM	31223460
PBMC	Antiviral assay			Antiviral activity in PBM cells expressed as IC50, IC50=0.002μM	ChEMBL
HepG2.2.15	Antiviral assay			Antiviral activity against hepatitis B virus in human hepatoma cell line (2.2.15 cells), EC50=0.01μM	ChEMBL
HepG2.2.15	Function assay			Effective concentration necessary to decrease extracellular Hepatitis B virus DNA levels by 50% in human hepatoblastoma cell line (2.2.15 cells) in vitro, EC50=0.038μM	ChEMBL
PBMC	Function assay			Compound was tested for its anti-HIV activity against HIV-1 LAI in human peripheral blood mononuclear (PBM) cells, EC50=0.06μM	ChEMBL
HepG2.2.15	Function assay			Effective concentration necessary to decrease extracellular Hepatitis B virus DNA levels by 90% in human hepatoblastoma cell line (2.2.15 cells) in vitro, EC90=0.16μM	ChEMBL
HepG2.2.15	Function assay			Tested for the effective concentration required to inhibit HBV in HepG2.2.15 human liver cells, EC50=0.2μM	ChEMBL
PBMC	Antiviral assay			Antiviral activity in PBM cells, IC50=0.21μM	ChEMBL
PBMC	Antiviral assay			Antiviral activity in PBM cells expressed as IC50, IC50=0.21μM	ChEMBL
MT-4	Antiviral assay			Antiviral activity in MT-4 cells, IC50=0.37μM	ChEMBL
MT-4	Antiviral assay			Antiviral activity in MT-4 cells expressed as IC50, IC50=0.37μM	ChEMBL
MT-4	Antiviral assay			Antiviral activity in MT-4 cells expressed as IC50, IC50=0.61μM	ChEMBL
MT-4	Function assay			Compound was tested for its anti-HIV activity in acutely infected MT-4 cells, EC50=7μM	ChEMBL
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生物活性

製品説明

Targets

Reverse transcriptase ^[1]

In Vitro
In vitro	Lamivudine’s anti- HBV activity, like its anti-HIV activity, has been shown to depend on the ability of LMV-TP to serve as both substrate and inhibitor of the DNA- and RNA-dependent polymerase activities of the HBV P gene product. Lamivudine owes its activity to the remarkably broad substrate specificity of deoxycytidine kinase and the unusual substrate preference of the HBV polymerases for dNTPs with the unnatural L-conformation, whereas the anti-HBV activity of PCV appears to depend on several factors including optimal phosphorylation (sufficient for antiviral activity but not cytotoxicity) by key cellular enzymes, the long intracellular half-life of PCV-TP and the ability of PCV-TP to inhibit the HBV RT priming reaction as well as RT and DNA polymerase activity. ^[1] Lamivudine and Penciclovir inhibits duck hepatitis B virus (DHBV) replication to a comparable extent when used alone, and in combination, the two nucleoside analogs acts synergistically over a wide range of clinically relevant concentrations. Lamivudine combined with Penciclovir is more effective in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV than either drug alone. ^[2] Lamivudine inhibits p24 antigen production by HIV-I in PBMC, with ED50s ranging from 0.07 μM to 0.2 μM. ^[3]
細胞実験	細胞株	Neonatal rat ventricular cardiomyocytes
	濃度	5 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentrations of drug for 24 h.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06056596	Recruiting	Retinal Detachment\|Rhegmatogenous Retinal Detachment	University of Wisconsin Madison	January 30 2024	Early Phase 1
NCT04133012	Completed	HIV-1 Infection	ANRS Emerging Infectious Diseases\|ViiV Healthcare	February 10 2020	Not Applicable

参考
[1] Shaw T, et al. J Viral Hepat, 1999, 6(2), 89-106. [2] Colledge D, et al. Hepatology, 1997, 26(1), 216-225. [3] Merrill DP, et al. J Infect Dis, 1996, 173(2), 355-364. [4] Kashyap S, et al. Front Cardiovasc Med. 2021 Apr 9;8:634774. [5] Li Z, et al. Asian J Pharm Sci, 11 (5) (2016), pp. 641-647. + 展開

参考

+ 展開

化学情報

分子量	229.26	化学式	C₈H₁₁N₃O₃S
CAS No.	134678-17-4	SDF	Download Lamivudine SDFをダウンロードする
Smiles	C1C(OC(S1)CO)N2C=CC(=NC2=O)N
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 : 45 mg/mL ( (196.28 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 : 45 mg/mL

Ethanol : 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。

技術サポート

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Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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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):