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In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-dependently inhibit high-fat diet intake and reduce body weight.
In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-dependently inhibit high-fat diet intake and reduce body weight.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 μg | ¥ 1,410 | 35日内发货 | |
1 mg | ¥ 2,660 | 35日内发货 | |
5 mg | ¥ 11,000 | 35日内发货 |
产品描述 | In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-dependently inhibit high-fat diet intake and reduce body weight. |
靶点活性 | DAGLα:0.69 μM (IC50) |
分子量 | 478.62 |
分子式 | C25H48FO5P |
CAS No. | 1572051-31-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | DMSO: Soluble |
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