| Chemical Properties | Back Directory | [Boiling point ]
558.9±50.0 °C(Predicted) | [density ]
1.214±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 25 mg/ml; DMF:PBS (pH 7.2) (1:6): 0.14 mg/ml; DMSO: 20 mg/ml; Ethanol: 2.5 mg/ml | [form ]
A crystalline solid | [pka]
9.51±0.18(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
MAGL inhibitor compound 23 is an inhibitor of monoacylglycerol lipase (MAGL; IC50 = 80 nM).1 It is selective for MAGL over cannabinoid receptor 1 (CB1), CB2, fatty acid amide hydrolase (FAAH), α/β-hydrolase domain-containing protein 6 (ABHD6), and ABHD12 (IC50s = >10 μM). MAGL inhibitor compound 23 inhibits the growth of HCT116, MDA-MB-231, Caov-3, OVCAR-3, and SKOV3 cells (IC50s = 21, 7.9, 25, 57, and 15 μM, respectively) but not MRC5 cells (IC50 = >100 μM). It increases the levels of 2-arachidonoyl glycerol (2-AG; ) in mouse brain and plasma when administered at a dose of 50 mg/kg. | [Uses]
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays[1]. | [in vivo]
MAGL (compound 23) (50 mg/kg; a single i.p.) increases the 2-AG level in plasma and brain, and does not alter anandamide (AEA), arachidonic acid and prostaglandin levels in plasma and brain of mice[1]. | Animal Model: | Male C57BL6 mice, 8-10 weeks old[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; once | | Result: | Increased 2-AG levels in the brain and plasma. |
| [References]
1. Granchi, C., Lapillo, M., Glasmacher, S., et al. Optimization of a benzoylpiperidine class identifies a highly potent and selective reversible monoacylglycerol lipase (MAGL) inhibitor J. Med. Chem. 62(4),1932-1958(2019). |
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