MAGL-IN-1

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

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-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].

MAGL-IN-14 (compound 2) serves as a potent MAGL inhibitor, exhibiting IC50 values of 0.00289 μM in HEK293 cells and 0.002 μM in PC3 cells [1].

MAGL-IN-15 (Compound 6), a MAGL inhibitor, holds potential for research into diseases and disorders associated with the regulation of endocannabinoid system signaling activities [1].

MAGL-IN-18 (compound 118) serves as a highly potent inhibitor of Monoacylglycerol lipase (MAGL), demonstrating an IC 50 value of 0.03nM.

MAGL-IN-19 (compound 7o) is a highly effective and selective inhibitor of MAGL.

MAGL-IN-13 (compound(3R,4S)-5v) is a selective, irreversible MAGL inhibitor with IC50 values of 0.026 nM for mMAGL, 0.021 nM for hMAGL, and 0.24 nM for rMAGL. Additionally, MAGL-IN-13 is capable of crossing the blood-brain barrier.

MAGL-IN-16 (compound 27) is an orally active, selective, and reversible MAGL inhibitor with an IC50 value of 10.3 nM. It increases 2-AG levels in vivo and exhibits antidepressant effects in mouse models of chronic restraint stress-induced depression.

PROTACMAGLdegrader-1 is an orally active PROTAC agent that simultaneously targets both monoacylglycerol lipase (MAGL) and the E3 ubiquitin ligase MDM2. It functions by degrading MAGL and inhibiting the interaction between MDM2 and p53. Additionally, PROTACMAGLdegrader-1 has partial blood-brain barrier (BBB) penetration and can induce apoptosis in glioblastoma stem cells (GSC).

OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microMing activities in

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-2, a potent and reversible inhibitor of FAAH and MAGL, demonstrates oral activity and the ability to cross the blood-brain barrier. It exhibits IC50 values of 11 nM for FAAH and 36 nM for MAGL (Ki values of 28 nM and 60 nM, respectively). This compound shows promise for neuropathic pain research, without impairing locomotion [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].