KT172

KT172 is a non-selective inhibitor of diacylglycerol lipase alpha (DAGLalpha) and DAGLbeta. It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Cay-10008650) in HEK293T cell membranes expressing recombinant DAGLalpha or DAGLbeta (IC50s = 140 and 60 nM, respectively). KT172 also inhibits alpha/beta-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 (Cay-62160) and subsequently reduces arachidonic acid (Cay-90010, Cay-90010.1, Cay-10006607), prostaglandin E2 (PGE2, Cay-14010), and PGD2 (Cay-12010) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.Formal Name: [4-(2'-methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylmethyl)-1-piperidinyl]-methanone. CAS Number: 1402612-56-9. Molecular Formula: C28H28N4O2. Formula Weight: 452.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5mg/mL, DMSO: 10mg/mL, DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL. lambdamax: 268 nm. SMILES: O=C(N1N=NC(C2=CC=C(C3=C(OC)C=CC=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4. InChi Code: InChI=1S/C28H28N4O2/c1-34-27-13-6-5-12-25(27)22-14-16-23(17-15-22)26-20-32(30-29-26)28(33)31-18-8-7-11-24(31)19-21-9-3-2-4-10-21/h2-6,9-10,12-17,20,24H,7-8,11,18-19H2,1H3. InChi Key: MXVVJNJNDCJCFS-UHFFFAOYSA-N.