Elbasvir

Elbasvir is a direct-acting antiviral drug that potently inhibits hepatitis C virus (HCV) non-structural protein 5A (NS5A) with an EC50 value of 2.2 pM in Huh7 human liver cancer cells expressing pH77S.3/GLuc2A, a cell-culture adapted HCV16 genotype 1a derivative and luciferase reporter, following a 48-hour exposure in vitro. NS5A is essential for HCV RNA synthesis and viral assembly, and elbasvir inhibits the assembly of new viral replicase complexes when used at a concentration of 50 pM. It exhibits potent inhibitory activity against a broad range of HCV genotypes with EC50 values of 0.0002-34 nM in Huh7 cells expressing replicons of HCV genotype 4 NS5A and EC50 values of less than 0.2 nM for replicons from all other tested genotypes except 2b. Formulations containing elbasvir have been used alone and in combination with NS3/4A protease inhibitors in the treatment of HCV.Formal Name: N,N'-[[(6S)-6-phenyl-6H-indolo[1,2-c][1,3]benzoxazine-3,10-diyl]bis[1H-imidazole-5,2-diyl-(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]bis-carbamic acid, C,C'-dimethyl ester. CAS Number: 1370468-36-2. Synonyms: MK-8742. Molecular Formula: C49H55N9O7. Formula Weight: 882.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMSO: 20 mgm/l, Ethanol: 33 mg/ml, Ethanol:PBS (pH 7.2)(1:2): 0.33 mg/ml. lambdamax: 284, 352, 369 nm. SMILES: O=C([C@H](C(C)C)NC(OC)=O)N(CCC1)[C@@H]1C(N2)=NC=C2C(C=C3)=CC4=C3N([C@H](C5=CC=CC=C5)OC6=C7C=CC(C8=CN=C([C@@H]9CCCN9C([C@@H](NC(OC)=O)C(C)C)=O)N8)=C6)C7=C4. InChi Code: InChI=1S/C49H55N9O7/c1-27(2)41(54-48(61)63-5)45(59)56-20-10-14-37(56)43-50-25-34(52-43)30-17-19-36-32(22-30)23-39-33-18-16-31(24-40(33)65-47(58(36)39)29-12-8-7-9-13-29)35-26-51-44(53-35)38-15-11-21-57(38)46(60)42(28(3)4)55-49(62)64-6/h7-9,12-13,16-19,22-28,37-38,41-42,47H,10-11,14-15,20-21H2,1-6H3,(H,50,52)(H,51,53)(H,54,61)(H,55,62)/t37-,38-,41-,42-,47-/m0/s1. InChi Key: BVAZQCUMNICBAQ-PZHYSIFUSA-N.