[CAS NO. 1535212-07-7] Voxilaprevir

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PRODUCTS SPECIFICATIONS [1535212-07-7]

Catalog

HY-19840

Brand

MCE

CAS

1535212-07-7

DESCRIPTION [1535212-07-7]

Overview

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

For research use only. We do not sell to patients.

Summary

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] .

IC50 & Target

Hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease ^[1]

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 ^[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.

Clinical Trial

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 115.08 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Cyclopropanecarboxamide, N-[[[(1R,2R)-2-[5,5-difluoro-5-(3-hydroxy-6-methoxy-2-quinoxalinyl)pentyl]cyclopropyl]oxy]carbonyl]-3-methyl-L-valyl-(3S,4R)-3-ethyl-4-hydroxy-L-prolyl-1-amino-2-(difluoromethyl)-N-[(1-methylcyclopropyl)sulfonyl]-, cyclic (1→2)-ether, (1R,2R)-

Voxilaprevir

GS 9857