| 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 inhibits HCV replication with a mean IC50 of 0.6 μM, PSI-6130-TP inhibits HCV replicase with a mean IC50 of 0.34 μM. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3′-end of the negative strand of the HCV genome with an IC50 of 0.13 μM and Ki of 0.023 μM. PSI-6130 is metabolized to two pharmacologically active species in primary human hepatocytes[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) |
| 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. |