MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC 50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain. In Vitro MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC 50 >10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid