A potent in vitro inhibitor of sn-1 DAGLα (IC50 = 18 nM); blocks the hydrolysis of sn-1-oleoyl-2-AG

LEI-106 – 1 mg

Brand:
Cayman
CAS:
1620582-23-1
Storage:
-20
UN-No:
Non-Hazardous - /

In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; Item No. 62160) by attacking DAG at the sn-1 position. LEI-106 is a potent in vitro inhibitor of sn-1 DAGLα (IC50 = 18 nM).{26613} It blocks the hydrolysis of sn-1-oleoyl-2-AG, the natural substrate of DAGLα, with a Ki value of 0.7 µM.{26613} LEI-106 inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6 in mouse brain membrane homogenates and in HEK293T cell membrane preparations (Ki = 0.8 µM).{26613}  

 

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Description

A potent in vitro inhibitor of sn-1 DAGLα (IC50 = 18 nM); blocks the hydrolysis of sn-1-oleoyl-2-AG, the natural substrate of DAGLα, with a Ki value of 0.7 µM; inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6 in membrane preparations (Ki = 0.8 µM)

Formal name: ​N-[(3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-6-yl)sulfonyl]-N-[(4-phenoxyphenyl)methyl]-glycine

Synonyms: 

Molecular weight: 481.6

CAS: 1620582-23-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Lipid Biochemistry|Endocannabinoid/Endocannabinoid-like||Research Area|Lipid Biochemistry|Glycerolipids|Lipases

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