| Description | Elbasvir (MK-8742) is an inhibitor of nonstructural protein 5A (NS5A) of hepatitis C virus (HCV) being developed as a component of treatment regimens for chronic HCV infection. |
| In vitro | Elbasvir 在Huh7人类肝癌细胞中，对乙型肝炎病毒(HCV)非结构蛋白5A (NS5A)具有强力抑制作用，该细胞表达pH77S.3/GLuc2A（一种经细胞培养适应的HCV16基因型1a衍生物和荧光素酶报告基因），在体外暴露48小时后，EC50值为2.2 pM [1,2]。NS5A对于HCV RNA合成和病毒组装至关重要，而在50 pM浓度下使用elbasvir能抑制新的病毒复制复合体的组装 [2]。在表达HCV基因型4 NS5A复制子的Huh7细胞中，elbasvir对广泛的HCV基因型显示出强大的抑制活性，EC50值为0.0002-34 nM。Elbasvir 对所有其他已测试基因型的复制子（2b型除外）的EC50值小于0.2 nM [1,3,4]。含有elbasvir的配方已单独和联合使用NS3/4A蛋白酶抑制剂在HCV治疗中使用。 |
| Target activity | NS5A:2.2 pM (EC50) |
| Synonyms | MK-8742 |
| molecular weight | 882.02 |
| Molecular formula | C49H55N9O7 |
| CAS | 1370468-36-2 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (56.69 mM) |
| References | 1. Lahser, F.C., 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. 60(5), 2954-2964 (2016). 2. McGivern, et al. Kinetic analyses reveal potent and early blockade of hepatitis C virus assembly by NS5A inhibitors. Gastroenterology 147(2), 453-462 (2014). 3. Asante-Appiah, et al. Antiviral activity and resistance analysis of NS3/4A protease inhibitor grazoprevir and NS5A inhibitor elbasvir in Hepatitis C virus GT4 replicons. Antimicrob. Agents Chemother. 61(7), e00363-e00417 (2017). 4. Liu, R., et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir. Antimicrob. Agents Chemother. 59(11), 6922-6929 (2015). 6. 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 |