| Bioactivity | Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM[1]. | ||||||||||||
| Target | EC50: 92±5 nM (HCV) | ||||||||||||
| Invitro | When cathepsin A (CatA) is incubated with PSI-7977 or Sofosbuvir (PSI-7977) for 150 min, ~18-fold more PSI-352707 is formed when Sofosbuvir (PSI-7977) is the substrate compared with PSI-7976. Moreover, the catalytic efficiency for Sofosbuvir (PSI-7977) with CatA is ~30-fold higher than that for PSI-7976[1]. The genotype coverage of Sofosbuvir (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, Sofosbuvir (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). Sofosbuvir (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, Sofosbuvir (PSI-7977) produces anti-HCV activity with EC90 values 0.42 μM[3]. | ||||||||||||
| Name | Sofosbuvir | ||||||||||||
| CAS | 1190307-88-0 | ||||||||||||
| Formula | C22H29FN3O9P | ||||||||||||
| Molar Mass | 529.45 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. 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. [2]. 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. [3]. 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. [4]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065. |