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Sofosbuvir

MCE China：Sofosbuvir

Brand：MedChemExpress (MCE)

Cat. No.HY-15005

CAS：1190307-88-0

Synonyms：GS-7977; PSI-7977

Purity：99.97%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM.

In Vitro：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].

Cell Assay：Clone A cells are seeded into T75 flasks at about 5×106 cells/flask in Dulbecco's modified Eagle's medium (DMEM) containing 100 IU/mL Penicillin/100 μg/mL streptomycin and 10% fetal bovine serum. Similarly, human primary hepatocytes are seeded in cell plating medium into T75 flasks at about 5×106 cells/flask. After overnight incubation to allow the cells to attach, cells are incubated with 50 μM PSI-7851, PSI-7976, or Sofosbuvir (PSI-7977) in fresh medium for clone A cells or in cell maintenance medium for primary hepatocytes for up to 24 h at 37°C in a 5% CO2 atmosphere. The same procedures are applied when radiolabeled PSI-7851 is used in the study except that 1×106 cells per well are seeded into a 6-well plate, and the cells are incubated with 5 μM [3H]PSI-7851. At selected times, the medium is removed, and the cell layer is washed with cold phosphate-buffered saline (PBS). After trypsinization, cells are counted and centrifuged at 1,200 rpm for 5 min. The cell pellets are suspended in 1 mL of cold 60% methanol and incubated overnight at −20°C. The samples are centrifuged at 14,000 rpm for 5 min, and the supernatants are collected and dried using a SpeedVac concentrator and stored at −20°C until they are analyzed by high performance liquid chromatography (HPLC). Residues are suspended in 100 μL of water, and 50-μL aliquots are injected into HPLC[1].

IC50 & Target：EC50: 92±5 nM (HCV)[1] Cellular Effect Cell Line Type Value Description References

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References：

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]