Grazoprevir

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Chemical Structure| 1350514-68-9 同义名 : MK-5172
CAS号 : 1350514-68-9
货号 : A407625
分子式 : C38H50N6O9S
纯度 : 99%+
分子量 : 766.9
MDL号 : MFCD22741510
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • HCV Protease

    gt1a, Ki:0.01 nM

    gt2a, Ki:0.01 nM

  • HCV Protease

    gt1a, Ki:0.01 nM

    gt2a, Ki:0.01 nM
描述 Hepatitis C virus (HCV), a member of the Flaviviridae family of viruses in the Hepacivirus genus, is encoded by a 9.6-kb positive-strand RNA genome. MK-5172 is a selective inhibitor of HCV NS3/4a protease with broad activity across genotypes and resistant variants. In biochemical assays, MK-5172 demonstrated subnanomolar potency against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a. In chronically HCV-infected chimpanzees, the viral titer was suppressed an additional log with MK-5172 treatment (1 mg/kg; twice daily for 7 days). Liver drug concentrations 12 h after final doses were also ~4-fold higher with MK-5172, at 1.97 μM compared to 0.54 μM with vaniprevir, indicating better drug exposure at the site of HCV replication[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.30mL

0.26mL

0.13mL

6.52mL

1.30mL

0.65mL

13.04mL

2.61mL

1.30mL
参考文献

[1]Summa V, Ludmerer SW, et al. MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. Antimicrob Agents Chemother. 2012 Aug;56(8):4161-7.

[2]Harper S, McCauley JA, et al. Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ACS Med Chem Lett. 2012 Mar 2;3(4):332-6.

[3]Summa V, Ludmerer SW, McCauley JA, et al. MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants. Antimicrob Agents Chemother. 2012 Aug;56(8):4161-7