Boceprevir-d9 is intended for use as an internal standard for the quantification of boceprevir by GC- or LC-MS. Boceprevir is an inhibitor of hepatitis C virus (HCV) non-structural protease 3/4A (NS3/4A; Ki = 14 nM for the HCV genotype 1b enzyme).1 Boceprevir inhibits HCV replication in Huh7 cells (EC50 = 200 nM).2 It also inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro; Ki = 1.8 µM) and reduces cytopathic effects of SARS-CoV-2 in Vero cells (EC50 = 1.31 µM).3 Formulations containing boceprevir have been used in the treatment of HCV.
1.Malcolm, B.A., Liu, R., Lahser, F., et al.SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cellsAntimicrob. Agents Chemother.50(3)1013-1020(2006) 2.Maren, T.H.Carbonic anhydrase: Chemistry, physiology, and inhibitionPhysiol. Rev.47(4)595-781(1967) 3.Ma, C., Sacco, M.D., Hurst, B., et al.Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main proteaseCell Res.30(8)678-692(2020)