MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor ofcPLA2andiPLA2. MAFP is also a potent irreversible inhibitor ofanandamide amidase.

cPLA2, iPLA2^[1], Anandamide amidase^[2]

MAFP inhibits iPLA2, in a concentration-dependent manner with an IC₅₀of 5 μM after a 5 min preincubation at 40℃ in P388D1 cells. cPLA, is a phospholipid hydrolase using the hydroxyl of serine-228 residue as its catalytic nucleophile^[1]. MAFP is also an inhibitor of anandamide amidase and as a ligand for the CB1 cannabinoid receptor. MAFP demonstrates selectivity towards anandamide amidase for which it is approximately 3000 and 30000-fold more potent than it is towards chymotrypsin and trypsin, respectively. MAFP displaces [³H]CP-55940 binding to the CB1 cannabinoid receptor with an IC₅₀of 20 nM vs 40 nM for anandamide^[2].

370.48

Liquid

C₂₁H₃₆FO₂P

188404-10-6

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL(269.92 mM)

Methyl Acetate : ≥ 10 mg/mL(26.99 mM)

*"≥" means soluble, but saturation unknown.

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