Monoacylglycerol lipase inhibitor 1

Monoacylglycerol lipase inhibitor 1, also known as compound 13 [1], is a potent inhibitor of monoacylglycerol lipase.

MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.

N-Arachidonyl maleimide, a potent and irreversible monoacylglycerol lipase (MAGL) inhibitor, has an IC50 value of 140 nM [1].

LEI-106, a novel potent sn-1 DAGLalpha inhibitor, blocks the hydrolysis of sn-1-oleoyl-2-AG, inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6.

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.

FAAH MAGL-IN-1, also known as compound SIH 3, is a highly effective inhibitor of FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase). It exhibits IC50 values of 31 nM and 29 nM against FAAH and MAGL, respectively. This compound shows promising potential for advancing research in the field of neuropathic pain [1].

MAGL-IN-9, also referred to as compound 16, is a reversible inhibitor of monoacylglycerol lipase (MAGL) with a potent IC50 value of 2.7 nM [1].

MAGL-IN-8 (compound 13) is a reversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 2.5 ± 0.4 nM for human MAGL (hMAGL) [1].

MAGL-IN-11 (compound 29) is a selective, reversible inhibitor of monoacylglycerol lipase (MAGL) with potential applications in inflammation, cancer, and antioxidant research [1].

MAGL-IN-10, a reversible monoacylglycerol lipase (MAGL) inhibitor, exhibits favorable ADME properties and low in vivo toxicity. It is applicable in the study of cancer, neurological disorders, and inflammatory pathologies [1].

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) inhibites three SHs (ABHD6, ABHD11, and FAAH)