5.33088

Monoacylglycerol Lipase Inhibitor, Cpd21

• Synonyme(s) : Monoacylglycerol Lipase Inhibitor, Cpd21, MAGL Inhibitor, Cpd21
• Formule empirique (notation de Hill): C₂₆H₂₆O₄
• Numéro CAS: 1643657-35-5
• Poids moléculaire : 402.48
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 400 nM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
MAGL

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable