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- 2025年07月21日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
GS-441524
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1191237-69-0
- 规格：
100mg/50mg
| 规格： | 100mg | 产品价格： | ￥480.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥356.0 |
| 基本信息 | |
| CAS | No.1191237-69-0 |
| 英文名称 | GS-441524 |
| 分子式 | C12H13N5O4 |
| 分子量 | 291.26 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 靶点 | FIPV |
| 通路 | Anti-infection |
| 背景说明 | GS-441524 是一种具有药理活性的三磷酸核苷分子的分子前体，是猫传染性腹膜炎病毒 feline infectious peritonitis virus (FIPV) 的有效抑制剂。 |
| 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 EC50 of 0.78 μM.[1-3] |
| IC50 | EC50: 0.78 μM (FIPV)[1]. |
| 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[1]. |
| 细胞实验 | 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[1]. 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[3]. |
| 细胞实验 | To determine the toxicity of GS-441524 to CRFK cells n， CRFK cells are treated with 100， 33.3， 11.1， 3.7 or 1.2 μM GS-441524 for 24 h[1]. |
| 动物实验 | Cats[1] The 10 cats that developed disease signs are divided into two groups and treated with either 5 mg/kg (Group A; n=5) or 2 mg/kg (Group B; n=5) GS-441524 SC q24 h starting three days after unequivocal clinical evidence of FIP (days 12-19 post infection). The two cats that do not develop disease signs serve as controls for normal blood lymphocyte counts and rectal temperature[1]. |
| 数据来源文献 | [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. [3]. Victoria C. Yan， et al. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med. Chem. Lett. 2020. |
| 单位 | 瓶 |
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