SAR629

Names

[ Name ]:
SAR629

Biological Activity

[Description]:

SAR629 is a potent monoglyceride lipase (MGL) covalent inhibitor. SAR629 also inhibits 2-Arachidonoylglycerol (2-AG) degradation[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Metabolic Disease

[In Vitro]

SAR629 is a potent dual inhibitory action on MAGL and fatty acid amide hydrolase (FAAH). SAR629 inhibits rodent monoglyceride lipase (MGL) activity at subnanomolar potencies (IC50 values of 1.1 nM and 219 pM in rat and mouse brain membranes, respectively)[1].

[References]

[1]. Niina Aaltonen, et al. Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem Biol. 2013 Mar 21;20(3):379-90.

[2]. T Bertrand, et al. Structural basis for human monoglyceride lipase inhibition. J Mol Biol. 2010 Feb 26;396(3):663-73.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₉F₂N₅O

[ Molecular Weight ]:
383.39

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

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