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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.

MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL.
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).

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.

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