5.33088
Monoacylglycerol Lipase Inhibitor, Cpd21
Synonym(s):
Monoacylglycerol Lipase Inhibitor, Cpd21, MAGL Inhibitor, Cpd21
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About This Item
Empirical Formula (Hill Notation):
C26H26O4
CAS Number:
Molecular Weight:
402.48
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
form
solid
potency
400 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
A cell-permeable hexanoate ester compound that acts as a potent, selective, non-competitive, and reversible inhibitor of monoacylglycerol lipase (MAGL, Ki = 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
MAGL
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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