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Description

A benzoxazinone compound that acts as a potent inhibitor of human leukocyte elastase (IC50 = 29.5 nM), likely by covalently modifying active site serine. Shown to inhibit elastase secretion (IC50 = 80.8 nM), but not O2.- generation, in fLMP (Cat. No. 05-22-2500)-stimulated primary human neutrophil cultures. Reported to reduce neutrophil infiltration in lung after hemorrhagic shock in rats in vivo (1 mg/kg, i.v.)., A benzoxazinone compound that acts as a potent inhibitor of human leukocyte elastase (IC50 = 29.5 nM), likely by covalently modifying active site serine via a Michael addition-elimination reaction. Shown to inhibit medium elastase activity (IC50 = 80.8 nM), but not O2.- generation, in fLMP (Cat. No. 05-22-2500)-stimulated primary human neutrophil cultures. Reported to reduce neutrophil infiltration in lung after hemorrhagic shock in rats in vivo (1 mg/kg, i.v.) as assessed by increase in lung wet/dry ratio (0.75- vs. 1.23-fold increase, respectively, with or without treatment) and MPO activity (1.08- vs. 3.72-fold increase, respectively, with or without treatment).