CPLA2A INHIBITOR II PYRROPHENONE (C15-1305-018)

General description

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.

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.

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

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PLA2a

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Ono, T., et al. 2002. Biochem. J.363, 727.
Seno, K., et al. 2001. Bioorg. Med. Chem. Lett.11, 587.

Legal Information

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

Molecular Weight: 849.96. Empirical Formula: C₄₉H₃₇F₂N₃O₅S₂. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. potency: 4.2 . nM IC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.