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ChemicalBook CAS数据库列表 (2S,3S,4R,5R)-2-(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)-5-(羟基甲基)-3,4-吡咯烷二醇单盐酸盐

(2S,3S,4R,5R)-2-(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)-5-(羟基甲基)-3,4-吡咯烷二醇单盐酸盐

生物活性靶点体外研究体内研究 (2S,3S,4R,5R)-2-(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)-5-(羟基甲基)-3,4-吡咯烷二醇单盐酸盐试剂级价格

CAS号:222631-44-9
英文名:3,4-Pyrrolidinediol, 2-(4-amino-5H-pyrrolo3,2-dpyrimidin-7-yl)-5-(hydroxymethyl)-, monohydrochloride, (2S,3S,4R,5R)-
中文名:(2S,3S,4R,5R)-2-(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)-5-(羟基甲基)-3,4-吡咯烷二醇单盐酸盐
CBNumber:CB11211297
分子式:C11H16ClN5O3
分子量:301.73
MOL File:222631-44-9.mol

(2S,3S,4R,5R)-2-(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)-5-(羟基甲基)-3,4-吡咯烷二醇单盐酸盐化学性质

储存条件 :Store at -20°C
形态 :Solid
颜色 :White to off-white
水溶解性 :Water : ≥ 41 mg/mL (135.88 mM)

(2S,3S,4R,5R)-2-(4-氨基-5H-吡咯并[3,2-D]嘧啶-7-基)-5-(羟基甲基)-3,4-吡咯烷二醇单盐酸盐性质、用途与生产工艺

生物活性 Galidesivir (BCX4430) hydrochloride，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 hydrochloride 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 hydrochloride 对一些负义 RNA 病毒的 EC50 在 ~3 到 ~68 μM 之间。
靶点

RdRp inhibitor
体外研究

Cellular kinases phosphorylate Galidesivir (BCX4430) hydrochloride 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 hydrochloride effectively inhibits the infection of Vero cells with YFV. The EC ₅₀ determined by the neutral red uptake assay is 8.3 μg/ml (24.5 μM).

体内研究

Galidesivir (BCX4430) hydrochloride 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 hydrochloride has demonstrated pronounced efficacy.
Galidesivir hydrochloride (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.