KT172 – 10 mg

Brand:
Cayman
CAS:
1402612-56-9
Storage:
-20
UN-No:
Non-Hazardous - /

KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.{30430} 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.{51209} 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.{30430}  

 

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Description

A non-selective inhibitor of DAGLα and DAGLβ; inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol in HEK293T cell membranes expressing recombinant DAGα or DAGLβ (IC50s = 140 and 60 nM, respectively); inhibits ABHD6 (IC50 = 5 nM) and weakly inhibits MAGL (IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases (IC50s = 5 and 5,000 nM, respectively); restores nicotine-stimulated GABA release in isolated VTA dopamine neurons from rats chronically exposed to nicotine at 1 µM; decreases production of 2-arachidonoyl glycerol and subsequently reduces arachidonic acid, PGE2, and PGD2 in thioglycolate-stimulated peritoneal macrophages at 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

Synonyms: 

Molecular weight: 452.6

CAS: 1402612-56-9

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Glycerolipids|Lipases||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids