Monoacylglycerol Lipase Inhibitor, Cpd21

A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, K_i = 400 nM, IC₅₀ = 240 nM for hydrolysis of 2- arachidonoylglycerol (2-AG). Displays good selectivity over a broad panel of related enzymes and does not bind to CB1 and CB2 cannabinoid receptors (Ki >10 µM). Shown to inhibit mouse brain MAGL (IC₅₀ = 180 nM), but does not affect the activity of fatty acid amide hydrolaase (FAAH; IC₅₀ = 59 µM) in any significant manner. Improves the course of experimental autoimmune encephalitis (EAE) murine model of multiple sclerosis (5 mg/kg/day, i.p. for 21 days) without inducing any undesirable CB1-agonist-like activity.

MAGL inhibitor, Monoacylglycerol Lipase Inhibitor

Cell permeable: yes

Primary Target
MAGL

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)