cPLA2 and iPLA2 inhibitor, potent FAAH inhibitor
CAS：188404-10-6
分子式：C21H36FO2P
分子量：370.49
纯度：98%
存储：Store at -20°C

Background:

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]

Reference:
[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 of Inflammation 3, 307-308 (1994).
[2]. Lio, Y.C., Reynolds, L.J., Balsinde, J., et al. Irreversible inhibition of Ca2+-independent phospholipase A2 by methyl arachidonyl fluorophosphonate. Biochimica et Biophysica 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. The Journal of Biological Chemisty 271, 6758-6765 (1996).
[4]. Deutsch, D.G., Omeir, R., Arreaza, G., et al. Methyl arachidonyl fluorophosphonate: A potent irreversible inhibitor of anandamide amidase. Biochemical Pharmacology 53, 255-260 (1997).