加利西韦
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- CAS号:
- 249503-25-1
- 英文名:
- 3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-
- 英文别名:
- Immucillin-A;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)-
- 中文名:
- 加利西韦
- 中文别名:
- 加利西韦;加利司韦;加利地韦;化合物 T10491
- CBNumber:
- CB81211296
- 分子式:
- C11H15N5O3
- 分子量:
- 265.27
- MOL File:
- 249503-25-1.mol
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加利西韦化学性质
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沸点:
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661.2±55.0 °C(Predicted)
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密度:
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1.630±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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形态:
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Solid
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酸度系数(pKa):
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13.78±0.40(Predicted)
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颜色:
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White to off-white
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水溶解性:
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Water : 1.53 mg/mL (5.77 mM)
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加利西韦性质、用途与生产工艺
Galidesivir (BCX4430)，一种腺苷类似物和直接作用的抗病毒药物，能破坏病毒 RNA 依赖的 RNA 聚合酶 (RdRp) 活性。Galidesivir 在体外对多种 RNA 病毒病原体具有活性，包括丝状病毒和新兴的感染因子，如 MERS-CoV、SARS-CoV 和 SARS-CoV-2。Galidesivir 对一些负义 RNA 病毒的 EC50 在 ~3 到 ~68 μM。
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).
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Animal Model:
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Female Syrian golden hamsters (hamsters infected with YF virus)
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Dosage:
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4 mg/kg of body weight
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Administration:
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I.p.; twice daily for 7 days
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Result:
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Significantly improved the survival of hamsters infected with YFV.
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加利西韦
上下游产品信息
上游原料
下游产品
249503-25-1, 加利西韦 相关搜索:
- 抑制剂
- 生化试剂
- 加利地韦
- 化合物 T10491
- 加利西韦
- 加利司韦
- 249503-25-1
- (2S,3S,4R,5R)-2-(4-AMINO-5H-PYRROLO[3,2-D]PYRIMIDIN-7-YL)-5-(HYDROXYMETHYL)PYRROLIDINE-3,4-DIOL
- BCX4430 freebase
(Galidesivir)
- GALIDESIVIR (BCX 4430)
- Immucillin-A
- BCX4430 (freebase)
- 3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, (2S,3S,4R,5R)-