5.33088

Monoacylglycerol Lipase Inhibitor, Cpd21

• Sinónimos: Monoacylglycerol Lipase Inhibitor, Cpd21, MAGL Inhibitor, Cpd21
• Fórmula empírica (notación de Hill): C₂₆H₂₆O₄
• Número de CAS: 1643657-35-5
• Peso molecular: 402.48
• Código UNSPSC: 12352200

Propiedades

• Ensayo: ≥98% (HPLC)
• Nivel de calidad: 100
• Formulario: solid
• potencia: 400 nM K_i
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: off-white
• solubilidad: DMSO: 50 mg/mL
• temp. de almacenamiento: 2-8°C

Descripción

Descripción general

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

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
MAGL

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable