RO-9187 - Names and Identifiers
RO-9187 - Physico-chemical Properties
Molecular Formula | C9H12N6O5
|
Molar Mass | 284.22878 |
Melting Point | 188.0-189.0℃ |
Storage Condition | -20℃ |
In vitro study | RO-9187 is excellent substrates for deoxycytidine kinase and is phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. RO-9187 inhibits 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 (4′-azidocytidine) or 2′-C-methyl nucleosides. The formation of RO-9187-TP increased in a time- and dose-dependent manner. The maximal triphosphate concentration at 24 h is 87 pmol/106 cells with half-maximal triphosphate formation achieved at 12 μM RO-9187. |
In vivo study | 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 1.4 and 26 μM (390 and 7454 ng/mL) 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 2000 mg/kg/day. |
RO-9187 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 3.518 ml | 17.591 ml | 35.183 ml |
5 mM | 0.704 ml | 3.518 ml | 7.037 ml |
10 mM | 0.352 ml | 1.759 ml | 3.518 ml |
5 mM | 0.07 ml | 0.352 ml | 0.704 ml |
Last Update:2024-01-02 23:10:35
RO-9187 - Reference Information
biological activity | RO-9187 is a potent inhibitor of HCV Virus replication with an IC50 value of 171 nM. |
Target | IC50: 171 nM (HCV) |
Last Update:2024-04-10 22:29:15