monoacylglycerol lipase

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

JJKK 048 is a potent and selective MAGL inhibitor.

JZP-430 is an effective, highly selective, irreversible inhibitor of α β-hydrolase domain 6 (ABHD6) (IC50: 44 nM). It also shows ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

JNJ-42226314 is a highly selective non-covalent monoacylglycerol lipase (MAGL) inhibitor with anti-injury effects.JNJ-42226314 shows efficacy via endogenous cannabinoid-2-acryloylglycerol (2-AG) in models of neuropathic pain and inflammatory pain.

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

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).

WWL70 is a selective inhibitor of alpha beta hydrolase domain 6 with an IC50 of 70 nM.

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-20 (compound ±34) is a reversible inhibitor of monoacylglycerol lipase (MAGL). It exhibits significant antiproliferative activity against a range of cancer cell lines, including H460, HT29, CT-26, Huh7, and HCCLM-3.

MAGL-IN-21 (Compound (S)-6) is a selective inhibitor of monoacylglycerol lipase (MAGL) with an IC50 of 1.59 nM.

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

JZL195 is a selective and efficacious dual FAAH MAGL inhibitor.

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.

NF-1819 is a potent and selective irreversible MGL (β-lactam-based monoacylglycerol lipase) inhibitor. NF-1819 alleviates symptoms in a MS model in vivo and exhibits analgesic effects in an acute inflammatory pain model in vivo. NF-1819 displays high membrane permeability and brain penetrant.

URB602 is a specific monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL (IC50: 28±4 μM) through a noncompetitive mechanism.

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.

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).

ABX-1431 (Elcubragistat) is a selective and orally available CNS-penetrant monoacylglycerol lipase (MAGL MGLL) inhibitor (IC50: 14 nM).

Euphol, an alcohol tetracyclic triterpene, has a wide range of pharmacological properties and is considered to have anti-inflammatory action.

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.

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].

FAAH MAGL-IN-3 (Compound 10) is an irreversible dual inhibitor of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) with an IC50 of 179 nM for FAAH and 759 nM for MAGL. FAAH MAGL-IN-3 exhibited minimal permeability in the PAMPA (parallel artificial membrane permeability assay).

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.