Biochem/physiol Actions

Reversible: no

Cell permeable: yes

Primary TargetElastase

General 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).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Hsieh, P.W., et al. 2010. Eur. J. Med. Chem.45, 3111.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)