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Description: CB1-IN-1 (also known as DBPR211) is a novel, potent, peripherally restricted antagonist of the CB1R (cannabinoid 1 receptor) with Ki values of 0.3 nM and 21 nM for CB1R (EC50 of 3 nM) and CB2R, respectively. CB1-IN-1 has shown significant weight-loss effects and can decrease hepatic steatosis as well as insulin resistance in a diet-induced obese mice model. Therefore, it has great potential to be used in this related metabolic syndrome such as obesity. It also has favorable PK profiles including an extremely low brain to plasma ratio suggesting a low probability to cross BBB.
References: J Med Chem. 2013 Dec 27; 56(24):9920-33.
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