KML29

KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH[1][2].

Product Specifications

CAS Number

[1380424-42-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

MAGL

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/KML29.html

Concentration

10mM

Purity

99.64

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(N1CCC(C(C2=CC=C(OCO3)C3=C2)(C4=CC=C(OCO5)C5=C4)O)CC1)OC(C(F)(F)F)C(F)(F)F

Molecular Formula

C24H21F6NO7

Molecular Weight

549.42

Precautions

H302, H315, H319, H335

References & Citations

[1]Natsuo Ueda, et al. Discrimination between two endocannabinoids. Chem Biol. 2012 May 25;19 (5) :545-7.|[2]Jae Won Chang, et al. Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem Biol. 2012 May 25;19 (5) :579-88.|[3]B M Ignatowska-Jankowska, et al. In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects. Br J Pharmacol. 2014 Mar;171 (6) :1392-407.