KT109

KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM) . KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A) . KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-Arachidonoylglycerol (HY-W011051), Arachidonic acid (HY-109590) and eicosanoids in mouse peritoneal macrophages[1].

Product Specifications

CAS Number

[1402612-55-8]

UNSPSC

12352005

Hazard Statement

H302, H413

Target

DAGL; MAGL

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/kt109.html

Concentration

10mM

Purity

99.86

Solubility

DMSO : 20 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N1N=NC(C2=CC=C(C3=CC=CC=C3)C=C2)=C1)N4CCCCC4CC5=CC=CC=C5

Molecular Formula

C27H26N4O

Molecular Weight

422.52

Precautions

H302, H413

References & Citations

[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.|[2]Wilkerson JL, et al. Diacylglycerol lipase β inhibition reverses nociceptive behaviour in mouse models of inflammatory and neuropathic pain. Br J Pharmacol. 2016 May;173 (10) :1678-92.