1800327-36-9
Chemical Structure
LEI105
- CAS. Nr.: 1800327-36-9
- Formula:C25H24N2O2
- Molecular Weight:384.47
IUPAC Name: 6-phenyl-1-(6-(p-tolyl)oxazolo[4,5-b]pyridin-2-yl)hexan-1-one
InChIKey: XDHONXIOZAUYDB-UHFFFAOYSA-N
SMILES: O=C(C1=NC2=NC=C(C3=CC=C(C)C=C3)C=C2O1)CCCCCC4=CC=CC=C4
Biological Activity: LEI105 is a highly selective and reversible diacylglycerol lipase (DAGL) inhibitor that exhibits significant inhibitory activity against human DAGLα and DAGLβ (e.g., the pIC50 value against human DAGLα is 8.5, and the IC50 against human DAGLβ is 32 nM). LEI105 effectively reduces intracellular 2-arachidonoylglycerol levels and inhibits CB1 receptor-mediated short-term synaptic plasticity. LEI105 can be used to investigate the on-demand biosynthesis of 2-AG in retrograde signaling[1][2].
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LEI105 | LEI105 is a highly selective and reversible diacylglycerol lipase (DAGL) inhibitor that exhibits significant inhibitory activity against human DAGLα and DAGLβ (e.g., the pIC50 value against human DAGLα is 8.5, and the IC50 against human DAGLβ is 32 nM). LEI105 effectively reduces intracellular 2-arachidonoylglycerol levels and inhibits CB1 receptor-mediated short-term synaptic plasticity. LEI105 can be used to investigate the on-demand biosynthesis of 2-AG in retrograde signaling. | |||||||||||||||||||||
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- [1]. Berger N, et al. Inhibition of diacylglycerol lipase β modulates lipid and endocannabinoid levels in the human placenta. Frontiers in endocrinology. 2023;14:1092024. [Content Brief]
- [2]. Baggelaar MP, et al. Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons. Journal of the American Chemical Society. 2015 Jul 15;137(27):8851-7. [Content Brief]
Keywords
