Bioactivity | MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity[1][2]. |
Invitro | MI-1851 (0-100 μM, 2h, 24 h) does not affect PHH cells viability, and extracellular hydrogen peroxide production even at 100 μM but reduces CYP3A4 isoenzyme activity in PHH cells in a dose-dependent manner[1].MI-1851 (10-50 μM, 72 h) strongly inhibits the spread of SARS-CoV-2 and its proliferation in Calu-3 cells even at a low dose of 10 μM, which reduces the virus titer by 30 to 190-fold[2]. MI-1851 (compound 8) (0.5-16 μM, 48 h) inhibits DENV-2 and WNV replication with the EC50 values of 1.50 μM and 1.46 μM, respectively in huh-7 cells[3]. |
In Vivo | Animal Model: |
Name | MI-1851 |
CAS | 2417283-44-2 |
Formula | C34H53N15O6 |
Molar Mass | 767.88 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Erzsébet Pászti-Gere, et al. In vitro characterization of the furin inhibitor MI-1851: Albumin binding, interaction with cytochrome P450 enzymes and cytotoxicity. Biomed Pharmacother. 2022 Jul;151:113124. [2]. Dorothea Bestle, et al. TMPRSS2 and furin are both essential for proteolytic activation of SARS-CoV-2 in human airway cells. Life Sci Alliance. 2020 Jul 23;3(9):e202000786. [3]. Thuy Van Lam van, et al. The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin. ACS Med Chem Lett. 2021 Feb 9;12(3):426-432. |