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Sofosbuvir (GS-7977) is an HCV RNA replication inhibitor with an EC50 of 92 nM. Sofosbuvir (PSI-7977) is a uridine nucleotide analog as HCV NS5B polymerase inhibitor for the treatment of chronic hepatitis C virus (HCV) infection. Sofosbuvir (PSI-7977) is a more potent inhibitor of HCV RNA replication than PSI-7976. When CatA is incubated with PSI-7977 or PSI-7976, ~18-fold more PSI-352707 is formed when PSI-7977 is the substrate compared with PSI-7976, and the catalytic efficiency for PSI-7977 with CatA is ~30-fold higher than that for PSI-7976. However, CES1 preferentially hydrolyzes PSI-7976 over PSI-7977. Incubating clone A cells with PSI-7977 results in a higher concentration of PSI-7409 than that with PSI-7976. NS5B polymerase S282T mutation but not S96T mutation is resistant to PSI-7977 with EC90 of 7.8 μM. PSI-7977 has no cytotoxicity against Huh7, HepG2, BxPC3, and CEM cells even at concentrations up to 100 μM. PSI-7977 is active against genotype (GT) 1a, 1b, and 2a (strain JFH-1) replicons and chimeric replicons containing GT 2a (strain J6), 2b, and 3a NS5B polymerase. Cross-resistance studies using GT 1b replicons confirme that the S282T change conferres resistance to PSI-7977. Data from the JFH-1 replicon variants show that amino acid changes within the finger and palm domains together with S282T are required to confer resistance to PSI-7977, while the mutations on the thumb domain serve to enhance the replication capacity of the S282T replicons. PSI-7977 is currently being investigated in phase 3 clinical trials for the treatment of hepatitis C.
| Cell Experiment | |
|---|---|
| Cell lines | Huh7, HepG2, BxPC3, and CEM |
| Preparation method | Exposing cells to various concentrations of PSI-7977 for 8 days. At the end of the growth period, adding MTS dye from the CellTiter 96 AQueous One Solution Cell Proliferation Assay kit to each well, and incubating the plate for an additional 2 hours. Read the absorbance at 490 nm with a Victor3 plate reader using themedium only controlwells as blanks. determing the 50% inhibition value (IC50) by comparing the absorbance in wells containing cells and PSI-7977 to untreated cell control wells. |
| Concentrations | Dissolved in DMSO, final concentrations ~100 μM |
| Incubation time | 8 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 529.45 |
| Formula | C22H29FN3O9P |
| CAS Number | 1190307-88-0 |
| Solubility (25°C) | DMSO 80 mg/mL Water 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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