Description
VX-950 is a potent, small molecule, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3.4A serine protease with IC50 of 350 nM.
Alias
VX950, Telaprevir, LY-570310, MP-424
Storage
2 years -20centigrade Powder
Synonyms
VX950, Telaprevir, LY-570310, MP-424
Targets
HCV NS3-4A serine protease
Molecular Formula
C36H53N7O6
Chemical Name
(3S,3aS, 6aR)-2-[(2S)-2-[[(2S)-2-cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl] amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1, 2-dioxohexan-3-yl]-3,3a,4,5,6, 6a-hexahydro-1H-cyclopenta[c]pyrrole-3-carboxamide
Solubility
DMSO 136 mg/ml, Water
In vitro
VX-950 is a potent, small molecule, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3.4A serine protease. Although competitive with the peptide substrate in the active site, VX-950 exhibits apparent noncompetitive inhibition as a result of its tight binding properties and time-dependent inhibition mechanism. Incubation of the HCV Con1 subgenomic replicon cells with VX-950 results in a concentration-dependent decline of the HCV RNA level. The dominant resistance mutation observed against VX-950 was a substitution of Ala156 in the HCV NS3 protease domain with a serine. VX-950 demonstrates excellent antiviral activity both in genotype 1b HCV replicon cells with IC50 of 354 nM and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera with IC50 of 280 nM. VX-950 forms a covalent but reversible complex with the genotype 1a HCV NS3-4A protease in a slow-on, slow-off process with a steady-state inhibition constant Ki of 7 nM.
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