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Elbasvir

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Chemical Structure| 1370468-36-2 同义名 : MK-8742
CAS号 : 1370468-36-2
货号 : A155998
分子式 : C49H55N9O7
纯度 : 99%+
分子量 : 882.017
MDL号 : MFCD30829850
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(56.69 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Non-structural protein 5A (NS5A) is important for RNA synthesis and virus assembly making it as an attractive target for intervention in chronic Hepatitis C virus (HCV) infection[3]. Elbasvir is a small molecule inhibitor of NS5A of HCV being developed as a component of treatment regimens for chronic HCV infection. In the 3-day replicon assay, the EC90 of elbasvir was 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. The EC90 of elbasvir ranged from 0.01 to 0.02 nM for genotype 1a and 0.01 to 0.03 nM for genotype 1b. In a phase 1 study, elbasvir once daily for 5 days resulted in mean reductions in HCV RNA levels of 3.7-5.1 log10 IU/mL in patients with genotype 1a or 1b infections when given 5-50 mg/day and of ~3 log10 IU/mL in patients with genotype 3 when given 50 or 100 mg/day. In later phase 2 trials, treatment with elbasvir combined with grazoprevir (an investigational once-daily NS3/4A-protease inhibitor) ± ribavirin for 12 weeks produced SVR12 (sustained virologic response) rates of 87-98% for patients with genotype-1 infections[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.13mL

0.23mL

0.11mL

5.67mL

1.13mL

0.57mL

11.34mL

2.27mL

1.13mL
参考文献

[1]Lahser FC, Bystol K, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64.

[2]Liu R, Curry S, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-9.

[3]Lahser FC, Bystol K, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64

[4]Liu R, Curry S, McMonagle P, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-9