In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; Item No. 62160) by attacking DAG at the sn-1 position. LEI-106 is a potent in vitro inhibitor of sn-1 DAGLα (IC₅₀ = 18 nM).¹ It blocks the hydrolysis of sn-1-oleoyl-2-AG, the natural substrate of DAGLα, with a K_i value of 0.7 µM.¹ LEI-106 inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6 in mouse brain membrane homogenates and in HEK293T cell membrane preparations (K_i = 0.8 µM).¹

≥98%

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1.Janssen, F.J.,Deng, H.,Allarà, M., et al. Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6. Journal of Medicinal Chemistry 57(15), 6610-6622 (2014).