A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, Ki = 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
生化/生理作用
Cell permeable: yes
Primary Target MAGL
警告
Toxicity: Standard Handling (A)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他說明
Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany