2055172-60-4
Chemical Structure
(R)-KT109
- CAS No.: 2055172-60-4
- Formula:C27H26N4O
- Molecular Weight:422.52
IUPAC Name: (R)-(4-([1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl)(2-benzylpiperidin-1-yl)methanone
InChIKey: JKJMWHULJIOKPJ-RUZDIDTESA-N
SMILES: O=C(N1C=C(C2=CC=C(C3=CC=CC=C3)C=C2)N=N1)N4[C@H](CCCC4)CC5=CC=CC=C5
Biological Activity: (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[1][2][3].
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(R)-KT109 | (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. | |||||||||||||||||||||
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References
- [1]. Deng H, Kooijman S, Van Den Nieuwendijk A M C H, et al. Triazole ureas act as diacylglycerol lipase inhibitors and prevent fasting-induced refeeding[J]. Journal of Medicinal Chemistry, 2017, 60(1): 428-440.
- [2]. Deng H. Chemical tools to modulate endocannabinoid biosynthesis[J]. Medicinal Chemistry, 2013, 56: 8270-8279.
- [3]. Deng H, et al. Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-α and ABHD6 inhibitors. Medchemcomm. 2017;8(5):982-988. Published 2017 Mar 10. [Content Brief]
