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KT185 is an orally bioavailable inhibitor of alpha/beta-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes. It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG, Cay-62160) hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells). KT185 is selective for ABHD6 over diacylglycerol lipase beta (DAGLbeta) at 1 µM but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Cay-29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg. It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Cay-19112) on ABHD6.Formal Name: [4'-[1-[(2-phenyl-1-piperidinyl)carbonyl]-1H-1,2,3-triazol-4-yl][1,1'-biphenyl]-3-yl]-1-piperidinyl-methanone. CAS Number: 1472640-86-0. Molecular Formula: C32H33N5O2. Formula Weight: 519.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 279 nm. SMILES: O=C(N1N=NC(C2=CC=C(C3=CC=CC(C(N4CCCCC4)=O)=C3)C=C2)=C1)N5C(C6=CC=CC=C6)CCCC5. InChi Code: InChI=1S/C32H33N5O2/c38-31(35-19-6-2-7-20-35)28-13-9-12-27(22-28)24-15-17-25(18-16-24)29-23-37(34-33-29)32(39)36-21-8-5-14-30(36)26-10-3-1-4-11-26/h1,3-4,9-13,15-18,22-23,30H,2,5-8,14,19-21H2. InChi Key: SGQNTNACVSWXMA-UHFFFAOYSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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