O-7460 is a potent and selective DAGLα inhibitor, with an IC50 of 0.69 μM. O-7460 shows selectivity over onoacylglycerol lipase (MAGL), human CB1 and CB2 cannabinoid receptors. O-7460 can decrease HFD-caused an up-regulation of 2-AG levels.
体外研究:
O-7460 (10 μM; 20 min) decreases the Ionomycin (3 μM)-induced formation of 2-AG in N18TG2 cells.