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药物分子
MK-5172
| 品牌 | 厂商性质 | 产地 | 货期 |
|---|---|---|---|
| 阿拉丁 | 生产商 | 上海 | 现货 |
产品参数
| 货号 | CAS号 | 操作 |
|---|---|---|
| M124903-10mg | 1350514-68-9 | 询价 |
| M124903-1mg | 1350514-68-9 | 询价 |
| M124903-5mg | 1350514-68-9 | 询价 |
产品介绍
属性
| 溶解性 | 25°C: DMSO |
| 存贮条件 | 储存温度-20°C |
描述
| 产品介绍 | MK-5172是HCV NS3/4a蛋白酶抑制剂，对1b和1a亚型的IC50分别为7.4 nM和7 nM。 |
| 生化机理 |
in vitro: 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 . in vivo: In rats, MK-5172 showed a plasma clearance of 28 ml/min/kg and plasma half-life of 1.4 hr. When dosed p.o. at 5 mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7 uM.hr. The liver exposure of the compound was quite good (23 uM at 4 hr), and MK-5172 remained in liver 24 hr after a single p.o. 5 mg/kg dose. At 24 hr, the liver concentration of MK-5172 was 0.2 uM, 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 5 ml/min/kg and a 3 hr half-life after i.v. 2 mg/kg dosing and had good plasma exposure (AUC=0.4 uM.hr) after a p.o. 1 mg/kg dose. |
| 别名 | ;MK 5172;MK5172;Grazoprevir;(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 |
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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途