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1402612-56-9

1402612-56-9 Structure

1402612-56-9 Structure
IdentificationBack Directory
[Name]

Methanone, [4-(2'-Methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylMethyl)-1-piperidinyl]-
[CAS]

1402612-56-9
[Synonyms]

KT-172 (KT172)
KT172 >=98% (HPLC)
(2-benzylpiperidin-1-yl)-[4-[4-(2-methoxyphenyl)phenyl]triazol-1-yl]methanone
4-(2'-methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylmethyl)-1-piperidinyl]-methanone
Methanone, [4-(2'-Methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylMethyl)-1-piperidinyl]-
[Molecular Formula]

C28H28N4O2
[MOL File]

1402612-56-9.mol
[Molecular Weight]

452.55
Chemical PropertiesBack Directory
[storage temp. ]

2-8°C
[solubility ]

DMF:5.0(Max Conc. mg/mL);10.72(Max Conc. mM)
DMSO:10.0(Max Conc. mg/mL);21.43(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.25(Max Conc. mg/mL);0.55(Max Conc. mM)
[form ]

A crystalline solid
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Description]

KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ. It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol 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 and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E2 (PGE2; ), and PGD2 in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.
[Uses]

KT172 is a DAGLβ inhibitor with an IC50 value of 11 nM. KT172 can be used for the research of metabolic and inflammatory[1].
[References]

[1] Ku-Lung Hsu, et al. DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nat Chem Biol. 2012 Dec;8(12):999-1007. DOI:10.1038/nchembio.1105
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