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KT-172

Names

[ CAS No. ]:
1402612-56-9

[ Name ]:
KT-172

[Synonym ]:
(2-Benzylpiperidin-1-yl)(4-(2'-methoxy-[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)methanone
Cravatt Reagent
KT172
Methanone, [4-(2'-methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylmethyl)-1-piperidinyl]-
MFCD26960820
(2-Benzyl-1-piperidinyl)[4-(2'-methoxy-4-biphenylyl)-1H-1,2,3-triazol-1-yl]methanone
[4-(2'-Methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl][2-(phenylmethyl)-1-piperidinyl]-methanone

Biological Activity

[Description]:

KT-172 is a potent, selective inhibitor of DAGLβ with IC50 of 60 nM; displays selectivity over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11; disrupts the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids in mouse peritoneal macrophages; possesses one remaining off-target ABHD6 (IC50=5 nM).

[References]

References 1. Hsu KL, et al. Nat Chem Biol. 2012 Dec;8(12):999-1007. View Related Products by Target Diacylglycerol Lipase (DAGL)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
636.1±47.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H28N4O2

[ Molecular Weight ]:
452.547

[ Flash Point ]:
338.5±29.3 °C

[ Exact Mass ]:
452.221222

[ LogP ]:
4.89

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.641

Related Compounds