4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮
中文名称 | 4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 |
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中文同义词 | 4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮;化合物 T16774 |
英文名称 | RO 9187 |
英文同义词 | RO 9187;4-Amino-1-(4-C-azido-beta-D-arabinofuranosyl)-2(1H)-pyrimidinone;RO 9187;RO9187;4-Amino-1-(4-C -azido-β-D-arabinofuranosyl)-2 (1H )-pyrimidinone |
CAS号 | 876708-03-1 |
分子式 | C9H12N6O5 |
分子量 | 284.22878 |
EINECS号 | |
相关类别 | 代谢 |
Mol文件 | 876708-03-1.mol |
结构式 | ![]() |
4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 性质
熔点 | 188.0-189.0℃ |
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储存条件 | Store at -20°C |
溶解度 | H2O:7.14 mg/mL(25.12 mM;需要超声波) |
形态 | 粉末 |
颜色 | 浅黄至黄色 |
IC50: 171 nM (HCV)
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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-10870 | 4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 RO-9187 | 876708-03-1 | 5mg | 2000元 |
2024/08/19 | HY-10870 | 4-氨基-1-(4-C-叠氮基-BETA-D-呋喃阿拉伯糖基)-2(1H)-嘧啶酮 RO-9187 | 876708-03-1 | 10 mM * 1 mLin DMSO | 2200元 |