2070009-25-3

PSI-7977-¹³C-d₃ is intended for use as an internal standard for the quantification of PSI-7977 (Item No. 15402) 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). PSI-7977 is effective in vitro and in vivo.

PSI-7977-13CD3 is the isotope labelled analog of PSI-7977. PSI-7977 is a prodrug that is metabolized to the active antiviral agent 2''-deoxy-2''-α-fluoro-β-C-methyluridine-5''-monophosphate and is currently being investigated in phase 3 clinical trials for the treatment of hepatitis C. Studies have profiled PSI-7977 as a nucleotide inhibitor of hepatitis C virus, exerting selective inhibitory effects towards HCV NS5B polymerase.

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[2] MICHAEL J. SOFIA*. Discovery of a β-d-2′-Deoxy-2′-α-fluoro-2′-β-C-methyluridine Nucleotide Prodrug (PSI-7977) for the Treatment of Hepatitis C Virus[J]. Journal of Medicinal Chemistry, 2010, 53 19: 7202-7218. DOI: 10.1021/jm100863x
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