Galidesivir hydrochloride|222631-44-9|(BCX4430 hydrochloride; Immucillin-A hydrochloride)-陌孚医药/Medlife

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Galidesivir hydrochloride (Synonyms: BCX4430 hydrochloride; Immucillin-A hydrochloride)

目录号: PL11188 纯度: ≥99%

CAS No. :222631-44-9

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中文名称	Galidesivir hydrochloride
中文别名	(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;加利地韦盐酸盐;加利司韦盐酸盐
英文名称	Galidesivir hydrochloride
英文别名	3,4-Pyrrolidinediol,2-(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)-, hydrochloride(1:1), (2S,3S,4R,5R)-;3,4-Pyrrolidinediol,2-(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)-5-(hydroxymethyl)-,monohydrochloride, (2S,3S,4R,5R)- (9CI);BCX 4430;BCX-4430;Galidesivir hydrochloride;Immucillin-A hydrochloride
Cas No.	222631-44-9
分子式	C₁₁H₁₅N₅O₃^.HCl
分子量	301.73
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir hydrochloride inhibits some negative-sense RNA viruses with EC 50 s ranging from ~3 to ~68 μM.

性状

Solid

IC50 & Target[1][2]

RdRp inhibitor

体外研究(In Vitro)

Cellular kinases phosphorylate Galidesivir (BCX4430) hydrochloride to a triphosphate that mimics ATP; viral RNA polymerases incorporate the drugs monophosphate nucleotide into the growing RNA chain, causing premature chain termination.
Galidesivir hydrochloride 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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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). has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Taylor R, et al. BCX4430 - A broad-spectrum antiviral adenosine nucleoside analog under development for the treatment of Ebola virus disease. J Infect Public Health. 2016;9(3):220-226.
[2]. Elfiky AA, et al. ICN-1229, Remdesivir, PSI-7977, Galidesivir, and GS 1278 against SARS-CoV-2 RNA dependent RNA polymerase (RdRp): A molecular docking study. Life Sci. 2020 Mar 25:117592.

溶解度数据	In Vitro: DMSO : 105 mg/mL (347.99 mM; Need ultrasonic)H₂O : ≥ 41 mg/mL (135.88 mM)

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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