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KT-109

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18540
    KT109
    1 Publications Verification

    		 MAGL DAGL Metabolic Disease Inflammation/Immunology
    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 .
    KT109
  • HY-126031
    (R)-KT109

    		DAGL Inflammation/Immunology
    (R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .
    (R)-KT109
  • HY-126031A
    (S)-KT109

    		Endogenous Metabolite Others
    (S)-KT109 is an inhibitor of diacylglycerol lipase β (DAGLβ) with low inhibitory activity (IC50 = 39.81 nM). (S)-KT109 has relatively low inhibitory activity against DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol (IC50 = 794.3 nM). (S)-KT109 also has relatively low inhibitory activity against α/β-amidase domain-containing 6 (ABHD6) (IC50 = 630.9 nM) .
    (S)-KT109

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