| Description | PSI-6206 (RO 2433) (RO2433) is a selective HCV RNA polymerase inhibitor. |
| In vitro | PSI-6206 (RO2433) 在一个基于细胞的定量实时RT-PCR分析和替代性牛病毒性腹泻病毒(BVDV)分析中被测试其抗HCV活性，结果显示在任何分析中均未展现出活性或细胞毒性[1]。PSI-6130 (PSI-6130-TP) 与 RO2433 (RO2433-TP) 的5′-三磷酸（TP）形成随时间增加，并在48小时达到稳态水平。RO2433-TP 还能抑制由HCV复制子细胞分离出的原生HCV复制酶以及重组HCV聚合酶NS5B的RNA合成[2]。PSI-6206 (RO2433) 是PSI-6130的脱氨基衍生物，PSI-6130是一种强效且选择性的HCV NS5B聚合酶抑制剂[3]。 |
| Synonyms | 2'-deoxy-2'-fluoro-2'-C-methyluridine, RO 2433, GS-331007 |
| molecular weight | 260.22 |
| Molecular formula | C10H13FN2O5 |
| CAS | 863329-66-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (230.57 mM) |
| 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. |