Otenabant

• CAT Number: I004580
• CAS Number: 686344-29-6
• Molecular Formula: C25H25Cl2N7O
• Molecular Weight: 510.42
• Purity: ≥95%
• Synonyms: 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)purin-6-yl]-4-(ethylamino)piperidine-4-carboxamide
• Target: Cannabinoid Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 0.7 nM(Ki for binding)/0.2 nM (Ki for function) [1]

Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.IC50 Value: 0.7 nM(Ki for binding)/0.2 nM (Ki for function) [1]Target: CB1 receptorin vitro : Otenabant (CP-945,598) exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.7 nM) and functional assays (Ki = 0.2 nM). The compound has low affinity (Ki = 7600 nM) for human CB2 receptors[1]in vivo: Otenabant (CP-945,598) reverses four cannabinoid agonist-mediated CNS-driven responses (hypo-locomotion, hypothermia, analgesia, and catalepsy) to a synthetic cannabinoid receptor agonist. Otenabant (CP-945,598) exhibits dose and concentration-dependent anorectic activity in two models of acute food intake in rodents, fast-induced re-feeding and spontaneous, nocturnal feeding. Otenabant (CP-945,598) also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. CP-945,598 at 10 mg/kg promoted a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice[1]. After oral administration of a single dose of [(14)C]CP-945,598. Total mean recoveries of the radioactive dose were 97.7, 97.8, and 99.3% from mice, rats, and dogs respectively[2].Clinical trail: A phase 1 study of the roles of endocannabinoids in insulin secretion and action is recruiting.

Reference

[1]. John R. Hadcock, David A. Griffith, Dennis O. 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, Dennis O. Scott, David A. Griffith. 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, 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):234-7.