- MK 5172 hydrate
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- $7.00
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2020-02-14
- CAS:1350462-55-3
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 100kg
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| | MK 5172 hydrate Basic information |
| Product Name: | MK 5172 hydrate | | Synonyms: | MK 5172 hydrate;MK-5172 (hydrate);MK5172 hydrate;(33R,35S,91R,92R,5S)-5-(tert-butyl)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-17-methoxy-4,7-dioxo-2,8-dioxa-6-aza-1(2,3)-quinoxalina-3(3,1)-pyrrolidina-9(1,2)-cyclopropanacyclotetradecaphane-35-carboxamide Hydrate;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, hydrate (1:1), (1R,2S)-;GRAZOPREVIR HYDRATE;MK5172 HYDRATE;MK 5172 HYDRATE;Grazoprevir hydrate (MK-5172 hydrate);Anapivir | | CAS: | 1350462-55-3 | | MF: | C38H50N6O9S.H2O | | MW: | 784.91868 | | EINECS: | | | Product Categories: | | | Mol File: | 1350462-55-3.mol |  |
| | MK 5172 hydrate Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 50 mg/mL (63.70 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble) | | form | Powder | | color | White to off-white |
| | MK 5172 hydrate Usage And Synthesis |
| Uses | 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 Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively[1][2]. Grazoprevir hydrate inhibits SARS-CoV-2 3CLpro activity[3]. | | 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]. | | References | [1] Steven Harper , John A. McCauley , Michael T. Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ACS Med. Chem. Lett., 2012, 3 (4), pp 332-336
[2] Summa V, Ludmerer SW, McCauley JA, 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. DOI:10.1128/AAC.00324-12
[3] Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. DOI:10.1038/s41392-021-00628-x |
| | MK 5172 hydrate Preparation Products And Raw materials |
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