Otenabant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 CB1 受体拮抗剂，在结合和功能测定中 Ki 分别为 0.7 nM/0.12 nM；对人类 CB2 受体具有低亲和力 (Ki=7600 nM)；逆转大麻素激动剂介导的反应，减少啮齿动物的食物摄入量，增加能量消耗和脂肪氧化。

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.

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 | CP-945598 | CP945598

GPCR/G Protein

Cannabinoid Receptor

CB1

Metabolic Disease

Obesity

686344-29-6

510.4183

C25H25Cl2N7O

>98% (HPLC)

10 mM in DMSO

CCNC1(CCN(CC1)C2=NC=NC3=C2N=C(N3C4=CC=C(C=C4)Cl)C5=CC=CC=C5Cl)C(=O)N

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

(-20℃)

With Ice Pack

≥ 2 years