中文名 | RO-9187 |
英文名 | RO-9187 |
别名 | 化合物 T16774 4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 |
英文别名 | RO9187 RO-9187 RO 9187 4-Amino-1-(4-C-azido-beta-D-arabinofuranosyl)-2(1H)-pyrimidinone |
CAS | 876708-03-1 |
化学式 | C9H12N6O5 |
分子量 | 284.22878 |
熔点 | 188.0-189.0℃ |
存储条件 | -20℃ |
体外研究 | 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. |
体内研究 | 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. |
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 |
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