| Identification | Back Directory | [Name]
Methanone, (4-[1,1'-biphenyl]-4-yl-1H-1,2,3-triazol-1-yl)[2-(phenylMethyl)-1-piperidinyl]- | [CAS]
1402612-55-8 | [Synonyms]
KT-109
(KT109)
KT109 >=98% (HPLC)
(2-benzylpiperidin-1-yl)-[4-(4-phenylphenyl)triazol-1-yl]methanone
Methanone, (4-[1,1'-biphenyl]-4-yl-1H-1,2,3-triazol-1-yl)[2-(phenylMethyl)-1-piperidinyl]- | [Molecular Formula]
C27H26N4O | [MDL Number]
MFCD26960819 | [MOL File]
1402612-55-8.mol | [Molecular Weight]
422.52 |
| Chemical Properties | Back Directory | [Boiling point ]
637.3±53.0 °C(Predicted) | [density ]
1.19±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMF:10.0(Max Conc. mg/mL);23.67(Max Conc. mM)
DMSO:10.0(Max Conc. mg/mL);23.67(Max Conc. mM) | [form ]
powder | [pka]
-1.02±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
KT109 is a potent and selective inhibitor of?DAGLβ. | [Biochem/physiol Actions]
KT109 is a potent and selective inhibitor of Diacylglycerol lipase DAGLβ. Diacylglycerol lipases DAGLα and DAGLβ are serine hydrolases that biosynthesize the endocannabinoid 2-arachidonoylglycerol (2-AG). A lack of selective inhibitors has hampered study of these lipases. KT109 is a potent and selective DAGLβ inhibitor with an IC50 of 42 nM, ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against FAAH, MGLL and ABHD11, other key enzymes involved in endocannabinoid signaling. KT109 shows some inhibitory activity against PLA2G7 (IC50 = 1 μM) but no inhibitory activity against cytosolic phospholipase A2 (cPLA2 or PLA2G4A). The main off target inhibition against ABHD6 (IC50 = 16 nM) can be controlled for by use of the related compound, KT195, a potent (IC50 = 10 nM) and selective ABHD6 inhibitor with negligible activity against DAGLβ. KT109 disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages. |
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