249503-25-1
249503-25-1 结构式
基本信息
加利司韦
化合物 T10491
BCX4430 (freebase)
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
3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-
物理化学性质
常见问题列表
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. |