5.33088

Monoacylglycerol Lipase Inhibitor, Cpd21

• Synonym(s): Monoacylglycerol Lipase Inhibitor, Cpd21, MAGL Inhibitor, Cpd21
• Empirical Formula (Hill Notation): C₂₆H₂₆O₄
• CAS Number: 1643657-35-5
• Molecular Weight: 402.48
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• potency: 400 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, K_i = 400 nM, IC₅₀ = 240 nM for hydrolysis of 2- arachidonoylglycerol (2-AG). Displays good selectivity over a broad panel of related enzymes and does not bind to CB1 and CB2 cannabinoid receptors (Ki >10 µM). Shown to inhibit mouse brain MAGL (IC₅₀ = 180 nM), but does not affect the activity of fatty acid amide hydrolaase (FAAH; IC₅₀ = 59 µM) in any significant manner. Improves the course of experimental autoimmune encephalitis (EAE) murine model of multiple sclerosis (5 mg/kg/day, i.p. for 21 days) without inducing any undesirable CB1-agonist-like activity.

MAGL inhibitor, Monoacylglycerol Lipase Inhibitor

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MAGL

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Hernandez-Torres, G., et al. 2014. Angew Chem Int Ed Engl.53, in press.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable