Bioactivity | 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]. |
Name | MAGL-IN-12 |
CAS | 1352011-38-1 |
Formula | C16H17ClF6N2O4S |
Molar Mass | 482.83 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |