PSI-7977 | CAS:1190307-88-0

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Name:PSI-7977; GS 7977; sofosbuvir
Cat. No. :CS-0554
CAS No. :1190307-88-0
Formula:C22H29FN3O9P
M. Wt. : 529.45
Solubility:10 mM in DMSO

PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.IC50 & Target: EC50: 92±5 nM (HCV)[1]In Vitro: When cathepsin A (CatA) is incubated with PSI-7977 or PSI-7976 for 150 min, ~18-fold more PSI-352707 is formed when PSI-7977 is the substrate compared with PSI-7976. Moreover, the catalytic efficiency for PSI-7977 with CatA is ~30-fold higher than that for PSI-7976[1]. The genotype coverage of PSI-7977 by using GT 1b (Con1)-, 1a (H77)-, and 2a (JFH-1)-derived replicons and GT 1b chimeric replicons containing the NS5B region from the J6 GT 2a isolate and from GT 2b and GT 3a patient isolates is evaluated, PSI-7977 inhibits the replication of these replicons with similar EC50s (between 16 and 48 nM), and is especially active against the chimeric replicon containing the J6 NS5B (EC50=4.7 nM). PSI-7977 inhibits clone A (GT 1b) wild-type and S282T replicons with EC90 values of 0.42 and 7.8 μM, respectively[2]. In the clone A replicon assay, PSI-7977 produces anti-HCV activity with EC90 values 0.42 μM[3].

Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47. Lam AM, et al. Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus. Antimicrob Agents Chemother. 2012 Jun;56(6):3359-68. Sofia MJ, 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 virus. J Med Chem. 2010 Oct 14;53(19):7202-18.