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MAGL-IN-12

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].

Product Specifications

CAS Number

1352011-38-1

UNSPSC

12352005

Target

MAGL

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/magl-in-12.html

Solubility

10 mM in DMSO

Smiles

ClC1=CC=C(C=C1)S(NCC2CCN(CC2)C(OC(C(F)(F)F)C(F)(F)F)=O)(=O)=O

Molecular Formula

C16H17ClF6N2O4S

Molecular Weight

482.83

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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