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±
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Grazoprevir potassium salt
CAS number:1206524-86-8(DMSO) molecular formula:C38H49KN6O9S
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| Chinese alias | 格拉瑞韦钾盐 | ||
| English alias | - | ||
| CAS number | 1206524-86-8(DMSO) | molecular formula | C38H49KN6O9S |
| molecular weight | 804.99 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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