324761

Elastase Inhibitor V

• Sinonimo/i: Elastase Inhibitor V, 2-(2-Bromophenyl)-5-chloro-3,1-benzoxazin-4-one
• Formula empirica (notazione di Hill): C₁₄H₇BrClNO₂
• Peso molecolare: 336.57
• Codice UNSPSC: 12352200
• NACRES: NA.54

Proprietà

• Saggio: ≥99% (HPLC)
• Livello qualitativo: 100
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated; protect from light
• Colore: off-white
• Solubilità: DMSO: 50 mg/mL (Use only fresh DMSO.)
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.).

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Elastase

Reversible: no

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable