Voxilaprevir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Voxilaprevir (GS-9857) 是一种有效的 HCV NS3/4A 蛋白酶抑制剂，与索磷布韦和维帕他韦联合用于治疗 HCV 感染。

Voxilaprevir (GS-9857)?is a potent HCV NS3/4A protease inhibitor that is used in combination with sofosbuvir and velpatasvir for treatment of HCV infection.HCV Infection Phase 2 Clinical(In Vitro):NS3/4A protease is essential for proteolytic cleavage of the HCV encoded polyprotein (intomature forms of NS3, NS4A, NS4B, NS5A and NS5B proteins) and hence for viral replication.In enzymatic assays using recombinant NS3 protease domains and isogenic NS4A peptide cofactors provided in trans. Voxilaprevir is against HCV genotype 1b and 3a NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively.In stable cell lines (Huh-7-Lunet or Huh7-1C cells) expressing renilla luciferase-encoding HCV replicons. Voxilaprevir exhibits potent pangenotypic antiviral activity with EC50 ranging from 0.33 to 6.6 nM across genotypes 1 to 6. Voxilaprevir is against HCV replicon strain DQ314805, H77, Con1, JFH-1, J6,J8 (full length) and HM568433, SA13 (NS3 Chimera) with IC50 values of 0.33 nM, 3.9 nM, 3.3 nM, 3.7 nM, 4.5 nM, 1.8 nM, and 6.6 nM, 1.9 nM, respectively.

NS3/4A protease is essential for proteolytic cleavage of the HCV encoded polyprotein (intomature forms of NS3, NS4A, NS4B, NS5A and NS5B proteins) and hence for viral replication.In enzymatic assays using recombinant NS3 protease domains and isogenic NS4A peptide cofactors provided in trans. Voxilaprevir is against HCV genotype 1b and 3a NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively.In stable cell lines (Huh-7-Lunet or Huh7-1C cells) expressing renilla luciferase-encoding HCV replicons. Voxilaprevir exhibits potent pangenotypic antiviral activity with EC50 ranging from 0.33 to 6.6 nM across genotypes 1 to 6. Voxilaprevir is against HCV replicon strain DQ314805, H77, Con1, JFH-1, J6,J8 (full length) and HM568433, SA13 (NS3 Chimera) with IC50 values of 0.33 nM, 3.9 nM, 3.3 nM, 3.7 nM, 4.5 nM, 1.8 nM, and 6.6 nM, 1.9 nM, respectively.

——

GS-9857 | GS9857

Microbiology/Virology

HCV

HCV

Infection

HCV Infection

1535212-07-7

868.94

C40H52F4N6O9S

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (115.08 mM)

COC(C=C1)=CC2=C1N=C(C(O[C@@H](C3)[C@@H](CC)[C@@H](C(N[C@]4(C(NS(=O)(C5(C)CC5)=O)=O)C[C@H]4C(F)F)=O)N3C6=O)=N2)C(F)(F)CCCC[C@H]7[C@@H](C7)OC(N[C@H]6C(C)(C)C)=O

(33R,34S,35S,91R,92R,5S)-5-(tert-butyl)-N-((1R,2R)-2-(difluoromethyl)-1-(((1-methylcyclopropyl)sulfonyl)carbamoyl)cyclopropyl)-34-ethyl-14,14-difluoro-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxamide

(-20℃)

With Ice Pack

≥ 2 years