Grazoprevir

• 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].

• Product Name Alternative:

  MK-5172

• UNSPSC:

  12352005

• Hazard Statement:

  H303, H320

• Target:

  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

• Purity:

  99.94

• 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 Formula:

  C38H50N6O9S

• Molecular Weight:

  766.90

• Precautions:

  H303, H320

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Citation 01:

  Antivir Res. 2019 Nov;171:104612.|Antiviral Res. 2017 Mar;139:18-24. |Antiviral Res. 2022 Jan:197:105224.|bioRxiv. 2023 Feb 27:2023.02.27.530290.|bioRxiv. 2023 Oct 26:2023.10.26.561921.|bioRxiv. 2024 Dec 3:2024.11.26.625483.|bioRxiv. 2024 Mar 12.|Cancer Cell. 2022 Nov 14;40 (11) :1294-1305.e4.|Cancer Immunol Res. 2021 Sep;9 (9) :999-1007.|Development. 2025 May 16:dev.204505.|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 Pharm Biomed Anal. 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 (Basel) . 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 Nov 14;40 (11) :1294-1305.e4.|Cancer Cell. 2024 Nov 11;42 (11) :1955-1969.e7.

• CAS Number:

  1350514-68-9