Gabexate mesylate is a competitive inhibitor of serine proteases that displays high selectivity for TMPRSS2 (Transmembrane protease serine 2) (IC50 = 130 nM) with little or no activity towards several MMPs, caspases and USPs (>> 10 μM). Gabexate mesylate was reported to decrease inflammatory cytokines production and be useful as an anticoagulant.
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The Journal of pharmacology and experimental therapeutics, 305(1), 298-305 (2003-03-22)
Gabexate mesilate, a synthetic protease inhibitor, was shown to be effective in treating patients with sepsis-associated disseminated intravascular coagulation in which tumor necrosis factor-alpha (TNF-alpha) plays a critical role. We demonstrated that gabexate mesilate reduced lipopolysaccharide (LPS)-induced tissue injury by
Although infection by SARS-CoV-2, the causative agent of coronavirus pneumonia disease (COVID-19), is spreading rapidly worldwide, no drug has been shown to be sufficiently effective for treating COVID-19. We previously found that nafamostat mesylate, an existing drug used for disseminated
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