monoacylglycerol

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.

1-Stearoyl-rac-glycerol is a monoacylglycerol that contains stearic acid at the sn-1 position. 1-Stearoyl-rac-glycerol levels are decreased in tumor tissue in a mouse model of azoxymethane-induced colorectal carcinogenesis. 1-Stearoyl-rac-glycerol has been used in the composition of transfersomes for transdermal delivery of doxorubicin in rats, leading to doxorubicin accumulation in lymph nodes, spleen, and heart.

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).

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).

JZL195 is a selective and efficacious dual FAAH MAGL inhibitor.

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).

ML-211 is a carbamate-based dual inhibitor of LYPLA1 (IC50 = 17 nM) and LYPLA2 (IC50 = 30 nM).

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

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.

MGAT2-IN-1 is an orally active monoacylglycerol acyltransferase (MGAT2)inhibitor (human and mouse MGAT2 with IC50 of 7.8 and 2.4 nM , respectively).

PF-06471553 is an effective and selective inhibitor of monoacylglycerol acyltransferase 3 (IC50: 92 nM).

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].

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.

1-Pentadecanoyl-rac-glycerol is a monoacylglycerol that contains pentadecanoic acid at the sn-1 position. It has been found in wheat bran extracts.1 1-Pentadecanoyl-rac-glycerol levels are increased in a HepaRG cell-based model of hepatic steatosis induced by BSA-conjugated palmitate.2 |1. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).|2. Brown, M.V., Compton, S.A., Milburn, M.V., et al. Metabolomic signatures in lipid-loaded HepaRGs reveal pathways involved in steatotic progression. Obesity (Silver Spring) 21(12), E561-E570 (2013).

1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fasting alter hepatic lipid droplet proteome and diacylglycerol species and prevent diabetes in NZO mice. Biochim. Biophys. Acta 1851(5), 566-576 (2015).2. Narváez-Rivas, M., Vicario, I.M., Constante, E.G., et al. Changes in the concentrations of free fatty acid, monoacylglycerol, and diacylglycerol in the subcutaneous fat of Iberian ham during the dry-curing process. J. Agric. Food Chem. 55(26), 10953-10961 (2007). 1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2 References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fasting alter hepatic lipid droplet proteome and diacylglycerol species and prevent diabetes in NZO mice. Biochim. Biophys. Acta 1851(5), 566-576 (2015).2. Narváez-Rivas, M., Vicario, I.M., Constante, E.G., et al. Changes in the concentrations of free fatty acid, monoacylglycerol, and diacylglycerol in the subcutaneous fat of Iberian ham during the dry-curing process. J. Agric. Food Chem. 55(26), 10953-10961 (2007).

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