5.30538

cPLA2α Inhibitor II, Pyrrophenone

• Synonym(e): cPLA2α Inhibitor II, Pyrrophenone, Phospholipase A2α Inhibitor
• Empirische Formel (Hill-System): C₄₉H₃₇F₂N₃O₅S₂
• CAS-Nummer: 341973-06-6
• Molekulargewicht: 849.96
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: powder
• Wirksamkeit: 4.2 nM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: off-white
• Löslichkeit: DMSO: 100 mg/mL
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
PLA2a

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable