MAFP (Methyl ArachIDOnyl Fluorophosphonate) 是选择性，针对活性位点，不可逆的 cPLA2 和 iPLA2 抑制剂。 MAFP也是一种有效的不可逆的 anandamide amidase 抑制剂。

MAFP is an effective irreversible inhibitor of anandamide amidase. MAFP is an active-site directed and irreversible inhibitor of cPLA2 and iPLA2.

In a concentration-dependent manner after a 5 min preincubation at 40°C in P388D1 cells, MAFP inhibits iPLA2 (IC50: 5 μM). MAFP is also an inhibitor of anandamide amidase and as a ligand for the CB1 cannabinoid receptor. MAFP shows selectivity towards anandamide amidase for which it is approximately 3000 and 30000-fold more potent than it is towards chymotrypsin and trypsin, respectively. cPLA is a phospholipid hydrolase using the hydroxyl of serine-228 residue as its catalytic nucleophile[1]. MAFP displaces [3H]CP-55940 binding to the CB1 cannabinoid receptor with an IC50 of 20 nM vs 40 nM for anandamide[2].

188404-10-6

C21H36FO2P

370.48

Methyl Arachidonyl Fluorophosphonate

Methyl Acetate:9.0 mg/mL (24.3 mM)
DMSO:90.0 mg/mL (242.9 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years