A selective inhibitor of DAGLβ (IC50 = 42 nM); disrupts the lipid network involved in macrophage inflammatory responses

KT109 – 10 mg

Brand:
Cayman
CAS:
1402612-55-8
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. KT109 is a selective inhibitor of DAGLβ with an IC50 value of 42 nM.{30430} It demonstrates ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11.{30430} KT109 has been shown to disrupt the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid (Item No. 90010) and eicosanoids, in mouse peritoneal macrophages.{30430}  

 

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Description

A selective inhibitor of DAGLβ (IC50 = 42 nM); disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages

Formal name: (4-[1,1′-biphenyl]-4-yl-1H-1,2,3-triazol-1-yl)[2-(phenylmethyl)-1-piperidinyl]-methanone

Synonyms: 

Molecular weight: 422.5

CAS: 1402612-55-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Lipid Biochemistry|Endocannabinoid/Endocannabinoid-like||Research Area|Lipid Biochemistry|Glycerolipids|Lipases||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids

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