Glecaprevir (Synonyms: ABT-493)
目录号: PL04764 纯度: ≥98%
CAS No. :1365970-03-1
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中文名称
Glecaprevir
中文别名
格来普韦
英文名称
Glecaprevir
英文别名
Glecaprevir API;(1R,2R)-N-[[[(1R,2R)-2-[[4,4-Difluoro-4-(3-hydroxy-2-quinoxalinyl)-2-buten-1-yl]oxy]cyclopentyl]oxy]carbonyl]-3-methyl-L-valyl-(4R)-4-hydroxy-L-prolyl-1-amino-2-(difluoromethyl)-N-[(1-methylcyclopropyl)sulfonyl]cyclopropanecarboxamide cyclic (1→2)-ether;A 1282576.0;ABT 493;Glecaprevir;K6BUU8J72P;(3aR,7S,10S,12R,21E,24aR)-7-tert-butyl-N-{(1R,2R)-2(difluoromethyl)-1-[(1-methylcyclopropane-1-;ABT-493
Cas No.
1365970-03-1
分子式
C38H46F4N6O9S
分子量
838.87
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Glecaprevir 是一种新型的 HCV NS3/4A 蛋白酶 (HCV NS3/4A protease) 抑制剂,其 IC50 值在 3.5 和 11.3 nM 之间。Glecaprevir 也是 SARS-CoV 3CLpro 的抑制剂,IC50 为 4.09 μM。
生物活性
Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC 50 values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CL inhibitor with an IC 50 of 4.09 μM.
性状
Solid
IC50 & Target[1][2]
IC50: 3.5~11.3 nM (HCV NS3/4A protease)
体外研究(In Vitro)
Glecaprevir inhibits the enzymatic activity of HCV genotype 1-6 NS3/4A proteases with half maximal inhibitory concentration (IC50) values ranging from 3.5 to 11.3 nM in a biochemical assay. Glecaprevir inhibites HCV subgenomic stable replicons containing proteases from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, 6a and 6e in Huh-7 cells with 50% effective concentration (EC50) values ranging from 0.21 to 4.6 nM. Glecaprevir is active against a replicon containing protease from genotype 3, the most difficult-to-treat HCV genotype, with an EC50 value of 1.9 nM, which is 10- and 44-fold lower than those for paritaprevir and grazoprevir, respectively. The median Glecaprevir EC50 values against replicons containing these genotype 1a, 1b, 2a, 2b, 3a, 4a, 4d, and 5a clinical samples are 0.08, 0.29, 1.6, 2.2, 2.3, 0.41, 0.17, and 0.12 nM, respe
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]. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir. Antimicrob Agents Chemother. 2017 Oct 30. pii: AAC.01620-17.
[2]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.
溶解度数据
In Vitro: DMSO : ≥ 83.3 mg/mL (99.30 mM)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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