Grazoprevir potassium salt

格拉瑞韦钾盐

Grazoprevir potassium salt

G655458-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K i s of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively Grazoprevir potassium salt inhibits SARS-CoV-2 3CL pro activity In Vitro In biochemical assays, Grazoprevir (MK-5172) is effective against a panel of major genotypes and variants engineered with common resistant mutations, with K i of 0.01± In Vivo Grazoprevir (MK-5172) demonstrates efficacy in vivo against chronic-HCV-infected chimpanzees . When dosed to dogs, Grazoprevir (MK-5172) shows low clearance of 5 mL/min/kg and a 3 h half-life after iv dosing and has good plasma exposure (AUC=0.4 μM h) after a 1 mg/kg oral dose. Dog liver biopsy studies showed that the liver concentration of Grazoprevir after the 1 mg/kg oral dose is 1.4 μM at the 24 h time point. Similar to its behavior in rats, Grazoprevir demonstrates effective partitioning into liver tissue and maintains high liver concentration, relative to potency, 24 h after oral dosing in dogs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:Ki: 0.01±

Grazoprevir 钾盐（MK-5172 钾盐）是一种丙型肝炎病毒 NS3/4a 蛋白酶的选择性抑制剂，在不同基因型和耐药变体中具有广泛的活性，其 K i s 分别为 0.01 nM（gt1b）、0.01 nM（gt1a）、0.08 nM（gt2a）、0.15 nM（gt2b）、0.01 nM（gt1b）、0.08 nM（gt2a）、0.15 nM（gt2b）、0.01 nM（gt1a）、0.08 nM（gt2a）。

1206524-86-8(DMSO)

C38H49KN6O9S

804.99 g/mol

CC(C)(C)C1C(=O)N2CC(CC2C(=O)NC3(CC3C=C)C(=O)[N-]S(=O)(=O)C4CC4)OC5=NC6=C(C=CC(=C6)OC)N=C5CCCCCC7CC7OC(=O)N1.[K+]