PSI-7977-13C-d3 is intended for use as an internal standard for the quantification of PSI-7977 by GC- or LC-MS. PSI-7977 is a phosphoramidate prodrug of PSI-7851, a nucleoside analog that, when phosphorylated, inhibits the RNA-dependent RNA polymerase of hepatitis C virus (EC50 = 92 nM).1,2,3 PSI-7977 is effective in vitro and in vivo.2,4,5
1.Murakami, E., Tolstykh, T., Bao, H., et al.Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977J. Biol. Chem.285(45)34337-34347(2010) 2.Sofia, M.J., Bao, D., Chang, W., et al.Discovery of a β-D-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virusJ. Med. Chem.53(19)7202-7218(2010) 3.Lam, A.M., Espiritu, C., Bansal, S., et al.Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virusAntimicrob. Agents Chemother.56(6)3359-3368(2012) 4.Gane, E.J., Stedman, C.A., Hyland, R.H., et al.Nucleotide polymerase inhibitor sofosbuvir plus ribavirin for hepatitis CN. Engl. J. Med.368(1)34-44(2013) 5.Lawitz, E., Mangia, A., Wyles, D., et al.Sofosbuvir for previously untreated chronic hepatitis C infectionN. Engl. J. Med.368(20)1878-1887(2013)