CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.
CAY10508
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产品编号 T84518Cas号 878533-35-8
CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.
CAY10508 is a potent and selective inverse agonist for the central cannabinoid (CB1) receptor with therapeutic potential for treating obesity and drug dependence, lacking psychotropic effects. It exhibits a Ki value of 243 nM and an EC50 of 195 nM. At a concentration of 10 µM, CAY10508 displaces [3H]-CP-55,940 with 100% efficacy at the CB1 receptor and 35% at the peripheral cannabinoid (CB2) receptor. Its inverse agonist activity at the CB1 receptor was confirmed through a [35S]-GTPγS binding assay.
化学信息
分子量
486.2
分子式
C21H14Br2N2O2
CAS No.
878533-35-8
储存&溶解度
存储
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
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