Cayman Act-373898, 5mg

KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ. It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Item No. ) 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. KT172 decreases production of 2-arachidonoyl glycerol (Item No. ) and subsequently reduces arachidonic acid (Item Nos. | | ), prostaglandin E₂ (PGE₂; Item No. ), and PGD₂ (Item No. ) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.

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