Identification | Back Directory | [Name]
1-Piperidinecarboxylic acid, 4-[[[(4-chlorophenyl)sulfonyl]amino]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester | [CAS]
1352011-38-1 | [Synonyms]
SAR127303 SAR-127303 SAR 127303 1-Piperidinecarboxylic acid, 4-[[[(4-chlorophenyl)sulfonyl]amino]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester | [Molecular Formula]
C16H17ClF6N2O4S | [MOL File]
1352011-38-1.mol | [Molecular Weight]
482.83 |
Hazard Information | Back Directory | [Description]
SAR127303 is a potent covalent MAGL inhibitor. SAR127303 behaves as a selective and competitive inhibitor of mouse and human MAGL, which potently elevates hippocampal levels of 2-AG in mice. In vivo, SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. | [Uses]
SAR127303 is an orally active, selective, competitive monoacylglycerol lipase (MAGL) covalent inhibitor with IC50s of 3.8 nM and 29 nM for mouse and human MAGL, respectively. SAR127303 potently elevates hippocampal levels of 2-AG in mice. SAR127303 decreased long term potentiation (LTP) of CA1 synaptic transmission and acetylcholine release in the hippocampus. SAR127303 produces antinociceptive effects in assays of inflammatory and visceral pain. SAR127303 slows down epileptogenesis[1]. | [References]
[1] Guy Griebel, et al. Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents. Sci Rep. 2015 Jan 6:5:7642. DOI:10.1038/srep07642 |
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