Biochem/physiol Actions

Primary TargetPLA2a

Cell permeable: yes

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

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

1 mg in Glass bottle

Warning

Toxicity: Standard Handling (A)