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Catalog: | HY-19840 |
Brand: | MCE |
CAS: | 1535212-07-7 |
MDL | - |
---|---|
Molecular Weight | 868.93 |
Molecular Formula | C40H52F4N6O9S |
SMILES | O=C([C@H]1N(C([C@@H](NC(O[C@H]2[C@H]3C2)=O)C(C)(C)C)=O)C[C@@](OC4=NC5=CC(OC)=CC=C5N=C4C(F)(CCCC3)F)([H])[C@H]1CC)N[C@]6([C@H](C(F)F)C6)C(NS(=O)(C7(CC7)C)=O)=O |
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity [1] . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with K i values of 0.038 nM and 0.066 nM, respectively [1] . Voxilaprevir is an orally active direct-acting antiviral agent ( DAA ) and can be used for HCV infection research [2] .
Hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease [1]
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
[1]
.
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 K
i
values of 0.038 nM and 0.066 nM, respectively
[1]
.
In stable cell lines (Huh-7-Lunet or Huh7-1C cells) expressing renilla luciferase-encoding HCV replicons. Voxilaprevir exhibits potent pangenotypic antiviral activity with EC
50
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 IC
50
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT02397707 | Gilead Sciences |
HCV Infection
|
March 24, 2015 | Phase 1 |
NCT02185794 | Gilead Sciences |
Hepatitis C Virus Infection
|
June 13, 2014 | Phase 1 |
NCT04695769 | Helwan University |
Chronic Hepatitis C
|
November 21, 2020 | Phase 4 |
NCT02402452 | Gilead Sciences |
HCV Infection
|
May 5, 2015 | Phase 1 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : ≥ 100 mg/mL ( 115.08 mM )
* "≥" means soluble, but saturation unknown.
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.1508 mL | 5.7542 mL | 11.5084 mL |
5 mM | 0.2302 mL | 1.1508 mL | 2.3017 mL |
10 mM | 0.1151 mL | 0.5754 mL | 1.1508 mL |
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution
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