同义名 :	MK-8742
	CAS号 :	1370468-36-2
	货号 :	A155998
	分子式 :	C49H55N9O7
	纯度 :	99%+
	分子量 :	882.02
	MDL号 :	MFCD30829850
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	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