Telaprevir

Telaprevir is an inhibitor of hepatitis C virus (HCV) nonstructural protease 3/4A (NS3/4A, Ki = 7 nM). It inhibits viral replication in genotype 1b HCV replicon cells and isolated human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50s = 354 and 280 nM, respectively). Telaprevir (10-300 mg/kg) reduces plasma levels of a secreted placental alkaline phosphatase (SEAP) reporter gene in a mouse model of HCV NS3/4A protease activity. Formulations containing telaprevir have been used in the treatment of HCV.Formal Name: (1S,3aR,6aS)-(2S)-2-cyclohexyl-N-(2-pyrazinylcarbonyl)glycyl-3-methyl-L-valyl-N-[(1S)-1-[2-(cyclopropylamino)-2-oxoacetyl]butyl]octahydro-cyclopenta[c]pyrrole-1-carboxamide. CAS Number: 402957-28-2. Synonyms: LY570310, VX-950. Molecular Formula: C36H53N7O6. Formula Weight: 679.9. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 3 mg/ml. lambdamax: 268 nm. SMILES: O=C(N[C@@H](C1CCCCC1)C(N[C@@H](C(C)(C)C)C(N2[C@H](C(N[C@H](C(C(NC3CC3)=O)=O)CCC)=O)[C@](CCC4)([H])[C@]4([H])C2)=O)=O)C5=NC=CN=C5. InChi Code: InChI=1S/C36H53N7O6/c1-5-10-25(29(44)34(48)39-23-15-16-23)40-33(47)28-24-14-9-13-22(24)20-43(28)35(49)30(36(2,3)4)42-32(46)27(21-11-7-6-8-12-21)41-31(45)26-19-37-17-18-38-26/h17-19,21-25,27-28,30H,5-16,20H2,1-4H3,(H,39,48)(H,40,47)(H,41,45)(H,42,46)/. InChi Key: BBAWEDCPNXPBQM-GDEBMMAJSA-N.