| Description |
MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells[1].
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| Related Catalog |
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| In Vitro |
MM3122 (0-1 μM) has inhibitory activity against HGFA, matriptase, hepsin and thrombin with the IC50 values of 32, 0.31, 0.19 and more than 20 nM, respectively[1]. MM3122 (0.1-100 μM) inhibits SARS-CoV-2 calu-3, VSV-SARS CoV-2 chimera calu-3 and MERS VSV pseudotype calu-3 with the EC50 values of 74, 0.43 and 0.87 nM, respectively[1].
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| In Vivo |
MM3122 (i.p., 0-100 mg/kg, daily, 7 days) has no adverse effects, no weight loss or changes in harvested organs (liver, spleen and kidney) compared to controls in NOD-scid IL2Rgnull (NSG) mice[1]. MM3122 (i.p., 16.7 mg/kg, once) has a half-life of 8.6 hours in plasma and 7.5 hours in lung of NSG mice[1].
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| References |
[1]. Matthew Mahoney, et al. A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells. Proc Natl Acad Sci U S A. 2021 Oct 26;118(43):e2108728118.
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