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GS-441524

目录号: PL11193 纯度: ≥99%

CAS No. :1191237-69-0

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中文名称	GS-441524
中文别名	瑞德西韦中间体
英文名称	GS-441524
英文别名	EVO984;EVO 984;GS441524;(2R,3R,4S,5R)-2-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile;GS 441524;BRDWIEOJOWJCLU-LTGWCKQJSA-N;(2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbonitrile;GS-441524;2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile;;(2R,3R,4S,5R)-2-(4-aminopyrrolo[1,2-f][1,2,4]triazin-7-yl)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-carbonitrile;1BQK176DT6;s6814;BCP29949-1;C22275;2-C-(4-Aminopyrrolo(2,1-f)(1,2,4)triazin-7-yl)-2,5-anhydro-D-altrononitrile;D-Altrononitrile, 2-C-(4-aminopyrrolo(2,1-f)(1,2,4)triazin-7-yl)-2,5-anhydro-;(2R,3R,4S,5R)-2-(4-Aminopyrrolo[2,1-;CID 44468216
Cas No.	1191237-69-0
分子式	C₁₂H₁₃N₅O₄
分子量	291.26
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

GS-441524 是 Remdesivir 的主要活性代谢物，活性更优于 Remdesivir ，感染病毒的原代人肺和猫细胞的细胞模型中显示出相似的活性。 GS-441524 对猫传染性腹膜炎病毒 (FIPV) 有较强的抑制作用，对应的 EC₅₀ 值为 0.78 μM。

生物活性

GS-441524, predominant metabolite of Remdesivir and superior to Remdesivir against Covid-19 , shows comparable efficacy in cell-based models of primary human lung and cat cells infected with coronavirus. GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC 50 of 0.78 μM.

性状

Solid

IC50 & Target[1][2]

EC50: 0.78 μM (FIPV).

体外研究(In Vitro)

The cells appear and grow normally at all concentrations of GS-441524 and fail to uptake the fluorescent dye CellTox Green at 24 h. The cytotoxic concentration-50% (CC50) is therefore>100 μM. The effective concentration-50% (EC50) of GS-441524 is calculated to be 0.78 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

All 10 treated cats have a rapid response to treatment and lymphocyte levels and rectal temperatures return to pre-infection levels and levels of the two asymptomatic cats. All ten of the once or twice treated cats have remained normal to date (more than eight months post infection). Injections cause a transient "stinging" reaction in some cats within 10 s of compound administration. Localized and transient pain is evidenced by unusual posturing, licking at the injection site and/or vocalizations that last for approximately 30-60 s after injection. Injection reactions are more pronounced in some animals relative to others and reactions are inconsistent from one injection to the next and decreas over time.
Remdesivi (IV injection) in NHP results in GS-441524 being present in serum at concentrations 1000-fold higher than Remdesivir throughout a 7-day treatment course.

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

ClinicalTrial

参考文献

[1]. Murphy BG, et al. The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. Vet Microbiol. 2018 Jun;219:226-233.
[2]. Katherine Yang, et al. What Do We Know About Remdesivir Drug Interactions? Clin Transl Sci. 2020 May 13;10.1111/cts.12815.

溶解度数据	In Vitro: DMSO : 83.33 mg/mL (286.10 mM; Need ultrasonic)配制储备液

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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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