| Description | RO-9187 is an effective HCV virus replication inhibitor(IC50: 171 nM). |
| In vitro | RO-9187 suppresses RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations with similar potencies, suggesting no cross-resistance with either R1479 or 2′-C-methyl nucleosides. RO-9187 is excellent substrates for deoxycytidine kinase and is phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. The formation of RO-9187-TP increased in a time- and dose-dependent manner [1]. |
| In vivo | Plasma exposures of RO-9187 in rats increase in a dose-dependent manner between 10 and 2000 mg/kg after oral dosing. Plasma concentrations of RO-9187 (1.4 and 26 μM ) are achieved in rats and dogs at the 10 mg/kg dose level, respectively. Plasma concentrations up to 57 μM are achieved in rats dosed with RO-9187 (2000 mg/kg/day)[1]. |
| Target activity | HCV:171 nM |
| molecular weight | 284.23 |
| Molecular formula | C9H12N6O5 |
| CAS | 876708-03-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 7.14 mg/mL (25.12 mM), Sonication is recommended. |
| References | 1. Klumpp K, et al. 2'-deoxy-4'-azido nucleoside analogs are highly potent inhibitors of hepatitis C virus replication despite the lack of 2'-alpha-hydroxyl groups. J Biol Chem. 2008 Jan 25;283(4):2167-75. |