加利西韦
| 中文名称 | 加利西韦 |
|---|---|
| 中文同义词 | 加利司韦;加利西韦;化合物 T10491 |
| 英文名称 | 3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)- |
| 英文同义词 | 3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-;BCX4430 (freebase);Immucillin-A;GALIDESIVIR (BCX 4430);BCX4430 freebase (Galidesivir);(2S,3S,4R,5R)-2-(4-AMINO-5H-PYRROLO[3,2-D]PYRIMIDIN-7-YL)-5-(HYDROXYMETHYL)PYRROLIDINE-3,4-DIOL |
| CAS号 | 249503-25-1 |
| 分子式 | C11H15N5O3 |
| 分子量 | 265.27 |
| EINECS号 | |
| 相关类别 | 生化试剂 |
| Mol文件 | 249503-25-1.mol |
| 结构式 |  |
加利西韦 性质
| 沸点 | 661.2±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.630±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 酸度系数(pKa) | 13.78±0.40(Predicted) |
| 水溶解性 | Water : 1.53 mg/mL (5.77 mM) |
RdRp
Cellular kinases phosphorylate Galidesivir (BCX4430) to a triphosphate that mimics ATP; viral RNA polymerases incorporate the drug's monophosphate nucleotide into the growing RNA chain, causing premature chain termination.
Galidesivir effectively inhibits the infection of Vero cells with YFV. The EC50 determined by the neutral red uptake assay is 8.3 μg/ml (24.5 μM).
Galidesivir (BCX4430) is active after intramuscular, intraperitoneal, and oral administration in a variety of experimental infections. In nonclinical studies involving lethal infections with Ebola virus, Marburg virus, Rift Valley fever virus, and Yellow Fever virus, Galidesivir has demonstrated pronounced efficacy.
Galidesivir (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF).
| Animal Model: | Female Syrian golden hamsters (hamsters infected with YF virus) |
| Dosage: | 4 mg/kg of body weight |
| Administration: | I.p.; twice daily for 7 days |
| Result: | Significantly improved the survival of hamsters infected with YFV. |