5.30538

cPLA2α Inhibitor II, Pyrrophenone

• Sinônimo(s): cPLA2α Inhibitor II, Pyrrophenone, Phospholipase A2α Inhibitor
• Fórmula empírica (Notação de Hill): C₄₉H₃₇F₂N₃O₅S₂
• Número CAS: 341973-06-6
• Peso molecular: 849.96
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• forma: powder
• potência: 4.2 nM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: off-white
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

Pyrrophenone is a cell-permeable, non-toxic, pyrolidine derivative that acts as a highly potent, and reversible inhibitor of cytosolic phospholipase A2a (cPLA2a; IC50 = 4.2 nM). Does not inhibit the activities of PLA IB and IIA groups even at higher concentrations (~250 µM). Unlike AACOCF3 (Cat. No. 100109), its action is shown to be rapid and does not require a pre-incubation period. Diminishes the release of arachidonic acid (IC50 = 24 nM), prostaglandin E2 (PGE2; IC50 = 25 nM) and leukotriene C4 (IC50 = 14 nM) in A23187 stimulated THP-1 cells. Its effects on production of PGE2 and thromboxane B2 are comparable to those of indomethacin. Also shown to inhibit the lysophospholipase and esterase activity of cPLA2&alpha.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
PLA2a

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras notas

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable