Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM. A 10 µM concentration of CAY10508 resulted in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and peripheral cannabinoid (CB2) receptors, respectively. A [35S]-GTPγS binding assay revealed the inverse agonist properties of CAY10508 at the CB1 receptor.
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Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
878533-35-8
SMILES
Brc1ccc(cc1)N1C(=O)C(c2ccccc2)N(c2ccc(Br)cc2)C1=O
Molecular Formula
C21H14Br2N2O2
Molecular Weight
486.2
Solubility
DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): .25 mg/ml,DMSO: 10 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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