產(chǎn)品描述: | Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively. |
靶點(diǎn): |
EC50: 4 nM (HCV 1a), 3 nM (HCV 1b), 3 nM (HCV 2a);HCVProtease |
體外研究: |
Elbasvir shows potent activity against genotype 1a and 1b replicons, with EC90 of 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. Elbasvir inhibits genotype 3 replicons with EC90 of 0.12 nM. Elbasvir (0.06 nM, 0.6 nM, and 6 nM) demonstrates dose-dependent suppression of resistant genotype 1a replicons, illustrated by the reductions in colony counts at higher doses. Elbasvir is highly potent against HCV replicons bearing NS5A sequences from GT1a, -1b, -2a(31L), -3a, -4a, -5a, and -6, with EC50s in the low-picomolar range |
參考文獻(xiàn): |
1. Liu R, 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):6922-6929. 2. Lahser FC, 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 A |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.134 ml |
5.669 ml |
11.338 ml |
5 mM |
0.227 ml |
1.134 ml |
2.268 ml |
10 mM |
0.113 ml |
0.567 ml |
1.134 ml |
50 mM |
0.023 ml |
0.113 ml |
0.227 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |