Telaprevir inhibits the hepatitis C virus NS3-4A serine protease, leading to the block of viral polyprotein processing. This eventually leads to a decrease of viral RNA replication, HCV RNA levels, as well as and protein levels in the Con1 (genotype 1b) subgenomic HCV replicon cells. This occurs in a time- and dose-dependent manner.

VX-950

≥98%

Telaprevir shows a significant time-dependent increase in inhibitory effect on the replication of HCV RNA with IC50 values of 574 nM, 488 nM, 210 nM and 139 nM for 24, 48, 72 and 120 hours incubation, respectively. On average it displays an IC50 of 354 nM and an average IC90 of 830 nM, respectively, from three independent experiments using 48 hours incubation.

≥100 mg/ml in DMSO <1 mg/ml in Water <1 mg/ml in Ethanol

Off-white powder

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Protease

Inhibitor