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KI3674CP94559810 mg$336

Chemical Characteristic

Product NameCP945598
SynonymsOtenabant
CAS No.919516-56-6
Molecular Weight 546.89
FormulaC25H25Cl2N7O
SmilesC1C(CCN(C1)c1ncnc2c1nc(n2c1ccc(cc1)Cl)c1ccccc1Cl)(C(=O)N)NCC
Chemical Structure

Biological activities

Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist. [1] Otenabant is progressed into Phase 3 human clinical trials as an oral agent for the treatment of obesity. It reduces acute food intake in rodents, decreases food intake and body weight in obese Beagle dogs and humans, and acutely stimulates energy expenditure in rats [2].In vitro, the IC50 of otenabant to CB1 is 0.7 nM(Ki for binding)/0.2 nM (Ki for function). In vivo, it can be used by 10 mg/kg in obese mice [3].

References

[1]. Hadcock JR, Griffith DA, Iredale PA, et al. Scott In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity. Biochemical and Biophysical Research Communications. 2010, 394:366-371.
[2]. Zhuang Miao, Scott DO, Griffith DA, et al. Excretion, Metabolism, and Pharmacokinetics of CP-945,598, a Selective Cannabinoid Receptor Antagonist, in Rats, Mice, and Dogs. Drug Metab. Dispos. 2011, 39: 568-578.
[3]. Griffith DA, Hadcock JR, Black SC, et al. Discovery of 1-[9-(4-chlorophenyl) -8-(2-chlorophenyl)- 9H-purin-6-yl] -4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. JMedChem. 2009, 52(2):234-237.

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