| Chemical Properties | Back Directory | [Boiling point ]
630.7±55.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
12.13±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain[1]. | [Biological Activity]
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain[1].
MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL[1]. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA)[1].
MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice[1]. | [in vivo]
MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice[1].
| [References]
[1]. Shuhei Ikeda, et al. Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H-benzo[ b][1,4]oxazin-6-yl Moiety. J Med Chem. 2021 Aug 12;64(15):11014-11044. |
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