Galidesivir

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Galidesivir

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

249503-25-1

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议
50mg	电议

产品名称

BCX4430
Immucillin-A

产品介绍

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。

生物活性

Galidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viralRNA-dependent RNA polymerase (RdRp)activity. Galidesivir 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 inhibits some negative-sense RNA viruses with EC₅₀s ranging from ~3 to ~68 μM^[1]^[2]^[3].

IC₅₀& Target

RdRp

体外研究
(In Vitro)

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^[1].
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)^[3].

体内研究
(In Vivo)

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^[1].
Galidesivir (4 mg/kg; i.p.; twice daily for 7 days) is effectively in a hamster model of yellow fever (YF)^[4].

Animal Model:	Female Syrian golden hamsters (hamsters infected with YF virus)^[4]
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.

Clinical Trial

分子量

265.27

性状

Solid

Formula

C₁₁H₁₅N₅O₃

CAS 号

249503-25-1

中文名称

加利司韦；加利地韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : 1.53 mg/mL(5.77 mM;Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.7697 mL	18.8487 mL	37.6974 mL
5 mM	0.7539 mL	3.7697 mL	7.5395 mL
10 mM	---	---	---

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。