Methyl arachidonyl fluorophosphonate (MAFP) is a selective, active-site directed, irreversible inhibitor of cPLA₂ and iPLA₂.^1,2,3 It inhibits A23187-induced arachidonic acid release from human platelets with an IC₅₀ value of 0.6 µM.¹ The IC₅₀ value for inhibition of iPLA₂ from P388D1 cells is 0.5 µM.² MAFP is a potent inhibitor of fatty acid amide hydrolase, exhibiting an IC₅₀ value of 2.5 nM. MAFP also binds to the CB₁ receptor in rat brain membrane preparations. The IC₅₀ values for MAFP and arachidonyl ethanolamide in this assay are 20 and 40 nM, respectively.⁴

1 Huang, Z., Liu, S., Street, I., et al. Methyl arachidonyl fluorophosphonate, a potent irreversible cPLA₂ inhibitor, blocks the mobilization of arachidonic acid in human platelets and neutrophils. Mediators Inflamm 3 307-308 (1994).

2 Lio, Y., Reynolds, L.J., Balsinde, J., et al. Irreversible inhibition of Ca2+-independent phospholipase A₂ by methyl arachidonyl fluorophosphonate. Biochim Biophys Acta 1302 55-60 (1996).

3 Balsinde, J., and Dennis, E.A. Distinct roles in signal transduction for each of the phospholipase A₂ enzymes present in P388D1 macrophages. J Biol Chem 271 6758-6765 (1996).

4 Deutsch, D.G., Omeir, R., Arreaza, G., et al. Methyl arachidonyl fluorophosphonate: A potent irreversible inhibitor of anandamide amidase. Biochem Pharmacol 53 255-260 (1997).

Balsinde, J., and Dennis, E.A. Distinct roles in signal transduction for each of the phospholipase A₂ enzymes present in P388D1 macrophages. J Biol Chem 271 6758-6765 (1996).

Huang, Z., Liu, S., Street, I., et al. Methyl arachidonyl fluorophosphonate, a potent irreversible cPLA₂ inhibitor, blocks the mobilization of arachidonic acid in human platelets and neutrophils. Mediators Inflamm 3 307-308 (1994).

Lio, Y., Reynolds, L.J., Balsinde, J., et al. Irreversible inhibition of Ca2+-independent phospholipase A₂ by methyl arachidonyl fluorophosphonate. Biochim Biophys Acta 1302 55-60 (1996).

Deutsch, D.G., Omeir, R., Arreaza, G., et al. Methyl arachidonyl fluorophosphonate: A potent irreversible inhibitor of anandamide amidase. Biochem Pharmacol 53 255-260 (1997).

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Methyl Arachidonyl Fluorophosphonate is available in the following screening library:

• Bio-active Lipid I Screening Library (96-Well)