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MAGL-IN-4 - 10mM in DMSO, high purity , CAS No.2135785-20-3(DMSO)

  • 10mM in DMSO
Item Number
M656572
Grouped product items
SKUSizeAvailabilityPrice Qty
M656572-1ml
1ml
Available within 8-12 weeks(?)
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$539.90
View related series
MAGL Metabolic Enzyme/Protease

Basic Description

Specifications & Purity10mM in DMSO
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
Product Description

MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC 50 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.

In Vitro

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 IC 50 >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). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Names and Identifiers

Canonical SMILES CC1=C(C=C(C=C1)COC2CN(C([C@H]3C[C@]4(COC(N4)=O)C3)=O)C2)Cl
Molecular Weight 364.82

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Solution Calculators