2-arachidonoylglycerol

In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand

2-Arachidonoylglycerol-d8 is the deuterated form of 2-Arachidonoylglycerol. 2-Arachidonoylglycerol serves as an endogenous cannabinoid ligand within the central nervous system.

2-Arachidonoylglycerol-d5 is the deuterated form of 2-Arachidonoylglycerol, which acts as an endogenous cannabinoid ligand within the central nervous system.

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.

Monoglyceridelipase is a crucial enzyme involved in lipid metabolism, catalyzing the hydrolysis of monoglycerides (especially 2-AG, or 2-arachidonoylglycerol) into glycerol and free fatty acids. By regulating the levels of 2-AG, this enzyme impacts neural signaling, pain perception, inflammatory responses, and metabolic processes.

MAGL-IN-222 (Compound ZQ-7) is a covalent inhibitor that targets monoacylglycerol lipase (MAGL), with an IC50 of 42.31 μM. It reduces the breakdown of 2-arachidonoylglycerol (2-AG), enhancing intracellular 2-AG levels, thereby inhibiting the proliferation and migration of MDA-MB-231 breast cancer cells. MAGL-IN-222 is applicable in breast cancer research and related diseases.

2-Palmitoylglycerol is an analog of 2-arachidonoylglycerol (2-AG) that does not bind positively to cannabinoid receptors and antagonizes 2-AG-mediated depolarization-induced suppression of excitation (DSE).

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).

O-Arachidonoyl glycidol (compound 1), a 2-arachidonoylglycerol (2-AG) analog, effectively inhibits the hydrolysis of cytosolic 2-oleoylglycerol (2-OG) with an IC50 value of 4.5 µM, and also blocks 2-OG and anandamide hydrolysis in membrane fractions with IC50 values of 19 µM and 12 µM, respectively [1].

2-Arachidonoylglycerol (2-AG) is identified as a more potent endogenous cannabinoid ligand compared to its analogue, 1-Arachidonoylglycerol (1-AG), exhibiting 10 to 100 times the ligand binding affinity and agonist activity at the CB1 receptor, thus making it a natural ligand. However, 2-AG's chemical instability leads to rapid isomerization to 1-AG (also referred to as 1(3)-AG) both in vitro and in vivo. This isomerization process, where 1-AG becomes a frequent contaminant in synthetic 1-AG preparations, significantly decreases their cannabinergic potency. Furthermore, 1-AG is characterized as a weak CB1 receptor agonist with potential for other pharmacological effects.