mouse magl

JW 642 is an effective inhibitor of monoacylglycerol lipase (MAGL) (IC50: 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively).

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human mouse rat MAGL (IC50: 5.9 15 43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

SA57 is a potent, selective inhibitor of FAAH(IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH).

SAR127303 is an effective covalent inhibitor of MAGL. SAR127303 behaves as a selective and competitive inhibitor of mouse and human MAGL.

CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50= 34.1 nM) that reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells at a concentration of 1 μM and increases levels of 2-arachidonoyl glycerol in mouse brain at 10 mg kg.

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

MJN110 (Cravatt Reagent) is a potent and selective MAGL inhibitor. Cravatt Reagent inhibits MAGL (IC50 = 9.1 nM). MJN110(Cravatt Reagent) Produces Opioid-Sparing Effects in a Mouse Neuropathic Pain Model.

MAGLi 432 is a potent, highly selective, non-covalent, reversible (MAGL) inhibitor that binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme), MAGLi 432 can be used to study neurological disorders such as chronic inflammation, multiple sclerosis, blood-brain barrier dysfunction, Alzheimer's disease and Parkinson's disease.

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.