Grazoprevir

Grazoprevir

• CAS Number: 1350514-68-9
• UNSPSC Description: Grazoprevir (MK-5172) 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 inhibits SARS-CoV-2 3CLpro activity[3].
• Target Antigen: HCV; HCV Protease; SARS-CoV
• Type: Reference compound
• Related Pathways: Anti-infection;Metabolic Enzyme/Protease
• Applications: COVID-19-anti-virus
• Field of Research: Infection
• Assay Protocol: https://www.medchemexpress.com/MK-5172.html
• Solubility: DMSO : 50 mg/mL (ultrasonic)|Ethanol : 66.67 mg/mL (ultrasonic)
• Smiles: COC1=CC2=C(N=C(CCCCC[C@@H]3C[C@H]3OC4=O)C(O[C@H]5CN(C([C@H](C(C)(C)C)N4)=O)[C@H](C(N[C@@]([C@@H]6C=C)(C6)C(NS(C7CC7)(=O)=O)=O)=O)C5)=N2)C=C1
• Molecular Weight: 766.90
• References & Citations: [1]Summa V, et al. 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.|[2]Harper S, et al. Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor. ACS Med Chem Lett. 2012 Mar 2;3(4):332-6.|[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.Antivir Res. 2019 Nov;171:104612.|Antiviral Res. 2017 Mar;139:18-24. |Antiviral Res. 2021 Dec 2;105224.|bioRxiv. 2023 Feb 27.|bioRxiv. 2023 Oct 26.|bioRxiv. 2024 Dec 3:2024.11.26.625483.|bioRxiv. 2024 Mar 12.|Cancer Cell. 2022 Aug 26;S1535-6108(22)00372-5.|Cancer Immunol Res. 2021 Jun 30.|Elife. 2020 Jun 9;9:e56469.|J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:15-24. |J Gastroenterol. 2019 May;54(5):449-458. |J Pharmaceut Biomed. 2020 Jan 30;178:112964.|Nat Biotechnol. 2019 Oct;37(10):1209-1216.|Nat Commun. 2020 Sep 4;11(1):4417.|Nat Methods. 2018 Jul;15(7):519-522.|Patent. US12065501.|Patent. US20180346589A1.|Patent. US20190010245A1.|Patent. US20220025003A1.|Pharmaceuticals. 2022 Feb 18;15(2):242.|Research Square Preprint. 2024 Jan 23.|Sci Rep. 2022 Jul 16;12(1):12197.|Sci Rep. 2019 Apr 5;9(1):5722.|Signal Transduct Target Ther. 2021 May 29;6(1):212.|University of Glasgow. 2024 Mar.|Cancer Cell. 2022 Aug 26;S1535-6108(22)00372-5.|Cancer Cell. 2024 Nov 11;42(11):1955-1969.e7.
• Shipping Conditions: Room Temperature
• Clinical Information: Launched