Drug intelligence / Profile preview

methyl arachidonyl fluorophosphonate

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Methyl arachidonyl fluorophosphonate (MAFP) is a potent, irreversible small molecule inhibitor of multiple serine hydrolases and proteases, primarily used as a research tool in lipid metabolism and endocannabinoid signaling. It acts as an active-site directed inhibitor that covalently binds to the catalytic serine residue of its targets, which include cytosolic phospholipase A2 (cPLA2), calcium-independent phospholipase A2 (iPLA2), and fatty acid amide hydrolase (FAAH), typically with low-nanomolar IC50 values. By inhibiting these enzymes, MAFP prevents the hydrolysis of phospholipids and the degradation of endocannabinoids like anandamide. Preclinical research has explored its potential in treating inflammatory conditions such as Crohn's disease by blocking PLA1A-mediated remodeling of phosphatidylcholine, as well as its antimicrobial activity against *Mycobacterium tuberculosis* through the inhibition of the thioesterase TesA. MAFP is explicitly labeled for research use only and is not intended for human therapeutic use.

Other names
methyl arachidonyl fluorophosphonate
02

Targets

TesA (Thioesterase 1)PLA2G7 (Platelet-activating factor acetylhydrolase)FAAHAcetylcholinesterasePLA2G4A (Cytosolic phospholipase A2 alpha)PLA1 (Phospholipase A1)PLA2 (Phospholipase A2 group IID)

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