Ensitrelvir fumarate (Synonyms: S-217622 fumarate)
目录号: PL11141 纯度: ≥99%
CAS No. :2757470-18-9
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中文名称
Ensitrelvir fumarate
英文名称
Ensitrelvir fumarate
英文别名
(E)-but-2-enedioic acid;6-[(6-chloro-2-methylindazol-5-yl)amino]-3-[(1-methyl-1,2,4-triazol-3-yl)met;Ensitrelvir fumarate
Cas No.
2757470-18-9
分子式
C26H21ClF3N9O6
分子量
647.95
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
Ensitrelvir (S-217622) fumarate 是第一个具有口服活性的,非共价的、非肽 SARS-CoV-2 3CL 蛋白酶抑制剂 (IC50=13 nM)。
生物活性
Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC 50 =13 nM).
性状
Solid
体外研究(In Vitro)
In a cytopathic effect (cpe)-inhibition assay of SARS-CoV-2 infected VeroE6/TMPRSS2 cells, Ensitrelvir fumarate shows the EC50 values are approximately 0.4 μM for both wild-type virus and Alpha, Beta, Gamma and Delta variants. EC50 values for SARS-CoV and MERS-CoV were 0.21 and 1.4 μM respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Ensitrelvir fumarate dose-dependently inhibits intrapulmonary replication of SARS-CoV-2 in mice. 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]. McKimm-Breschkin JL, et al. COVID-19, Influenza and RSV: Surveillance-informed prevention and treatment - Meeting report from an isirv-WHO virtual conference. Antiviral Res. 2022;197:105227.
[2]. Yuto Unoh, et al. Discovery of S-217622, a Non-Covalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19. bioRxiv 2022.01.26.477782.
溶解度数据
In Vitro: DMSO : 50 mg/mL (77.17 mM; Need ultrasonic)配制储备液
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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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