Elastase Inhibitor V-Calbiochem

C₁₄H₇BrClNO₂

336.57

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).
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.).

Cell permeable: yes
Primary Target
Elastase
Reversible: no

Toxicity: Standard Handling (A)

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

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

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

≥99% (HPLC)

100

solid

Calbiochem^®

OK to freeze
desiccated
protect from light

off-white

DMSO: 50 mg/mL (Use only fresh DMSO.)

ambient

2-8℃

25 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 2