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KT109

CAT: 0804-HY-18540-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-18540-01Size:5 mg
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Description
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 , Arachidonic acid (HY-109590) and eicosanoids in mouse peritoneal macrophages[1].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
DAGLβ