溶解性 | 25°C: DMSO |
存贮条件 | 储存温度-20°C |
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 |
MK-5172,Hepatitis C Virus NS3/4A Protease 抑制剂
MK-5172 (订货以英文为准)
编号:M124903
CAS号:1350514-68-9
分子式:C38H50N6O9S
分子量:766.90
产品名称 | MK-5172 |
中文名称 | MK-5172,Hepatitis C Virus NS3/4A Protease 抑制剂 |
CAS号 | 1350514-68-9 |
分子式(M.F.) | C38H50N6O9S |
分子量(M.W.) | 766.90 |
储存条件 | -20°C储存 |
信号词 | Warning |
危害声明 | H302-H319 |
警示性声明 | P305 + P351 + P338 |
WGK德国 | 3 |
搜索质检报告(COA)
搜索MSDS
相关产品