| Description | PSI-6130 (R 1656) is a potent and selective HCV NS5B polymerase inhibitor. PSI-6130 inhibits HCV replication with a mean IC50 of 0.6 μM. |
| In vitro | PSI-6130以平均IC50为0.6μM抑制HCV复制，PSI-6130-TP以平均IC50为0.34μM抑制HCV复制酶。在来源于HCV基因组负链3′端的异质聚合RNA模板上，PSI-6130-TP对重组HCV Con1 NS5B的抑制作用表现为IC50为0.13μM和Ki为0.023μM。在初级人类肝细胞中，PSI-6130被代谢为两种药理活性物种[1]。 |
| Target activity | HCV:0.6 μM |
| Synonyms | R 1656, 2'-去氧-2'-氟-2'-C-甲基胞苷 |
| molecular weight | 259.23 |
| Molecular formula | C10H14FN3O4 |
| CAS | 817204-33-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (192.88 mM), Sonication is recommended. |
| References | 1. Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13. 2. Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. |