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CAS No. : 1535212-07-7
MCE 国际站:Voxilaprevir
产品活性:Voxilaprevir (GS-9857) 是一种非共价、可逆的 HCV NS3/4A 蛋白酶抑制剂 (PI),具有泛抗病毒活性。Voxilaprevir 抑制基因型 1b 和 3a 野生型 NS3 蛋白酶的 Ki 值分别为 0.038 nM 和 0.066 nM。Voxilaprevir 是一种具有口服活性直接作用型抗病毒试剂 (DAA),可用于 HCV 感染的研究。
研究领域:Anti-infection | Metabolic Enzyme/Protease
作用靶点:HCV Protease
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.
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