| Identification | Back Directory | [Name]
MK5172 | [CAS]
1350514-68-9 | [Synonyms]
2)-ether
Grazoprevir
MK 5172; MK5172
Grazoprevir /MK5172
MK-5172 (Grazoprevir)
MK 5172 (10mM in DMSO)
GRAZOPREVIR;MK 5172;MK-5172
(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→
(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
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)-
(1R,18R,20R,24S,27S)-N-{(1R,2S)-1-[(Cyclopropylsulfonyl)carbamoyl]-2-vinylcyclopropyl}-7-methoxy-24-(2-methyl-2-propanyl)-22,25-dioxo-2,21-dioxa-4,11,23,26-tetraazapentacyclo[24.2.1.03,12.05,10.018,20]nonacosa-3,5,7,9,11-pentaene-27-carboxamide, potassiu
(1R,18R,20R,24S,27S)-N-{(1R,2S)-1-[(Cyclopropylsulfonyl)carbamoyl]-2-vinylcyclopropyl}-7-methoxy-24-(2-methyl-2-propanyl)-22,25-dioxo-2,21-dioxa-4,11,23,26-tetraazapentacyclo[24.2.1.03,12.05,10.018,20]nonacosa-3,5,7,9,11-pentaene-27-carboxamide, potassium salt | [Molecular Formula]
C38H50N6O9S | [MOL File]
1350514-68-9.mol | [Molecular Weight]
766.9 |
| Chemical Properties | Back Directory | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
≥38.35 mg/mL in DMSO; insoluble in H2O; ≥24 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
solid | [pka]
4.48±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MK 5172, also known as Grazoprevir, is a second-generation NS3/4A protease inhibitor that is often used in combination with the second-generation NS5A inhibitor, Elbasvir (E501010), for the treatment of hepatitis C virus infection. It is a COVID19-related research product. | [Definition]
ChEBI: An azamacrocyclic compound that is a hepatitis C protease inhibitor used in combination with elbasvir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults. | [in vivo]
Grazoprevir (MK-5172) demonstrates efficacy in vivo against chronic-HCV-infected chimpanzees[1]. 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[2]. |
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