324761

Elastase Inhibitor V

• Synonyme(s) : Elastase Inhibitor V, 2-(2-Bromophenyl)-5-chloro-3,1-benzoxazin-4-one
• Formule empirique (notation de Hill): C₁₄H₇BrClNO₂
• Poids moléculaire : 336.57
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.54

Propriétés

• Pureté: ≥99% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; desiccated; protect from light
• Couleur: off-white
• Solubilité: DMSO: 50 mg/mL (Use only fresh DMSO.)
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C

Description

Description générale

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.).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Elastase

Reversible: no

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable