KML29

Description: KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 µM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG, >50 µM, AEA). Target: Lipase. Smiles: OC(C1CCN(CC1)C(=O)OC(C(F)(F)F)C(F)(F)F)(c1ccc2OCOc2c1)c1ccc2OCOc2c1. References: Chang JW, et al. Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem Biol. 2012 May 25,19(5):579-588.