KT172

KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.¹ It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Item No. 10008650) in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC₅₀s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC₅₀ = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC₅₀ = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 µM.² KT172 decreases production of 2-arachidonoyl glycerol (Item No. 62160) and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E₂ (PGE₂; Item No. 14010), and PGD₂ (Item No. 12010) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.¹

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1. Hsu, K.L., Tsuboi, K., Adibekian, A., et al. DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nat. Chem. Biol 8(12), 999-1007 (2012).

2. Buczynski, M.W., Herman, M.A., Hsu, K.L., et al. Diacylglycerol lipase disinhibits VTA dopamine neurons during chronic nicotine exposure. Proc. Natl. Acad. Sci. USA 113(4), 1086-1091 (2016).