| Description | MAFP (Methyl Arachidonyl Fluorophosphonate) is an effective irreversible inhibitor of anandamide amidase. MAFP is an active-site directed and irreversible inhibitor of cPLA2 and iPLA2. |
| In vitro | 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]. |
| Synonyms | Methyl Arachidonyl Fluorophosphonate |
| molecular weight | 370.48 |
| Molecular formula | C21H36FO2P |
| CAS | 188404-10-6 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Methyl Acetate: 9.0 mg/mL (24.3 mM) DMSO: 90.0 mg/mL (242.9 mM) |
| References | 1. Lio YC, et al. Irreversible inhibition of Ca(2+)-independent phospholipase A2 by methyl arachidonyl fluorophosphonate. Biochim Biophys Acta. 1996 Jul 12;1302(1):55-60. 2. Deutsch DG, et al. Methyl arachidonyl fluorophosphonate: a potent irreversible inhibitor of anandamide amidase. Biochem Pharmacol. 1997 Feb 7;53(3):255-60. |