Otenabant hydrochloride

Research use only, not for human use.

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively.

A potent, and selective CB1 receptor antagonist with Ki of 0.7 nM/0.12 nM in binding and functional assays respectively; has low affinity (Ki=7600 nM) for human CB2 receptors; reverses cannabinoid agonist mediated responses, reduces food intake, and increases energy expenditure and fat oxidation in rodents.Obesity Phase 3 Discontinued(In Vitro):Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration.(In Vivo):Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. Otenabant (10 mg/kg, p.o.) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation.

Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration.

Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. Otenabant (10 mg/kg, p.o.) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation.

CP 945598 Hydrochloride | CP-945598 Hydrochloride | CP945598 Hydrochloride

GPCR/G Protein

Cannabinoid Receptor

hCB1|hCB2|rCB1

Metabolic Disease

Obesity

686347-12-6

546.8792

C25H26Cl3N7O

>98% (HPLC)

DMSO: 1 mg/mL

CCNC1(CCN(CC1)C1=NC=NC2=C1NC(N2C1=CC=C(Cl)C=C1)C1=CC=CC=C1Cl)C(N)=O

4-Piperidinecarboxamide, 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years