10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Grazoprevir hydrate (MK-5172 hydrate) 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 hydrate 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±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a), 0.07±0.01 nM (gt1b R155K ), 0.14±0.03 nM (gt1b D168V ), 0.30±0.04 nM (gt1b D168Y ), 5.3±0.9 nM (gt1b A156T ), and 12±2 nM (gt1b A156V ), respectively. In the replicon assay, Grazoprevir demonstrates subnanomolar to low-nanomolar EC 50 s against genotypes 1a, 1b, and 2a, with EC 50 s of 0.5±0.1 nM, 2±1 nM, and 2±1 nM for gt1b con1 , gt1a, and gt2a, respectively. Grazoprevir is potent against a panel of HCV replication mutants NS5A (Y93H) (EC 50 =0.7±0.3 nM), NS5B nucleosides (S282T) (EC 50 =0.3±0.1 nM), and NS5B (C316Y) (EC 50 =0.4±0.2). Grazoprevir (MK-5172) maintains the excellent potency against the gt 3a enzyme as well as a broad panel of mutant enzymes, has excellent potency in the replicon system [gt1b IC 50 (50% NHS)=7.4 nM; gt1a IC 50 (40% NHS)=7 nM], and shows excellent rat liver exposure. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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±<0.01 nM (gt1b), 0.01±0.01 nM (gt1a), 0.08±0.02 nM (gt2a), 0.15±0.06 nM (gt2b), 0.90±0.2 nM (gt3a)
| Isomeri SMILES | CC(C)(C)[C@H]1C(=O)N2C[C@@H](C[C@H]2C(=O)N[C@@]3(C[C@H]3C=C)C(=O)NS(=O)(=O)C4CC4)OC5=NC6=C(C=CC(=C6)OC)N=C5CCCCC[C@@H]7C[C@H]7OC(=O)N1.O |
|---|---|
| CAS alternativo | 1350462-55-3 |
| PubChem CID | 71576667 |
| Termini MeSH | cyclopropanecarboxamide, 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-ethenyl-, cyclic (1->2)-ether, (1R,2S)-;cyclopropanecarboxamide, N-( |
| Peso molecolare | 784.92 |
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