化学信息：
| 化学名 | (1R,2S)-N-[[[(1R,2R)-2-[5-(3-Hydroxy-6-methoxy-2-quinoxalinyl)pentyl]cyclopropyl]oxy]carbonyl]-3-methyl-L-valyl-(4R)-4-hydroxy-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenylcyclopropanecarboxamide cyclic (1→;2)-ether |
|
| 简称 | MK5172 | |
| 别名 |
Grazoprevir, MK 5172, MK5172 |
|
| 中文名 | N/A | |
| 化学式 | C38H50N6O9S | |
| 分子量 | 766.9 | |
| CAS号 | 1350514-68-9 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO10mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入0.65ml DMSO，或者每7.67mg加入1ml DMSO，配制成10mM溶液。SC3260-10mM用DMSO配制。 |
生物信息：
| 产品描述 | MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development. | ||||
| 信号通路 | Anti-infection; Metabolism; Proteases | ||||
| 靶点 | genotype 1b | genotype 1a | － | － | － |
| IC50 | 7.4nM | 7nM | － | － | － |
| 体外研究 | In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. | ||||
| 体内研究 | In rats, MK-5172 showed a plasma clearance of 28ml/min/kg and plasma half-life of 1.4hr. When dosed p.o. at 5mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7μM.hr. The liver exposure of the compound was quite good (23μM at 4hr), and MK-5172 remained in liver 24hr after a single p.o. 5mg/kg dose. At 24hr, the liver concentration of MK-5172 was 0.2μM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5ml/min/kg and a 3hr half-life after i.v. 2mg/kg dosing and had good plasma exposure (AUC=0.4μM.hr) after a p.o. 1mg/kg dose. | ||||
| 临床实验 | Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C. Phase 1. | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SC3260-10mM | MK5172 (HCV抑制剂) | 10mM×0.2ml |
| SC3260-5mg | MK5172 (HCV抑制剂) | 5mg |
| SC3260-25mg | MK5172 (HCV抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
