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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 µ,M). 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 µ,M). 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.