| Cas No.: | 863329-66-2 |
| Chemical Name: | N/A |
| Synonyms: | PSI-6206, RO-2433, PSI6206, RO2433 |
| SMILES: | C[C@]1([C@@H]([C@H](O[C@H]1N2C=CC(=O)NC2=O)CO)O)F |
| Formula: | C10H13FN2O5 |
| M.Wt: | 260.22 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM. |
| Target: | EC90:>100 μM (HCV replicon)[1] |
| In Vitro: | PSI-6206 (RO2433) is tested for anti-HCV activity in both a cell-based quantitative real-time RT-PCR assay and surrogate bovine viral diarrhea virus (BVDV) assays. PSI-6206 demonstrates no activity or cytoxicity in any assay[1]. The formation of the 5′-triphosphate (TP) of PSI-6130 (PSI-6130-TP) and RO2433 (RO2433-TP) increases with time and reached steady state levels at 48 h. RO2433-TP also inhibits RNA synthesis by the native HCV replicase isolated from HCV replicon cells and the recombinant HCV polymerase NS5B[2]. PSI-6206 (RO2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase[3]. |
| References: | [1]. Clark JL, et al. Design, Synthesis, and Antiviral Activity of 2'-Deoxy-2'-fluoro-2'-C-methyl-cytidine, a Potent Inhibitor of Hepatitis C Virus Replication. J Med Chem. 2005 Aug 25;48(17):5504-8. [2]. 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):29 [3]. Wang P, et al. An efficient and diastereoselective synthesis of PSI-6130: a clinically efficacious inhibitor of HCV NS5B polymerase. J Org Chem. 2009 Sep 4;74(17):6819-24. |

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