CP-945598CAS号： 686344-29-6分子式： C25H25Cl2N7O分子量： 510.42描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
Otenabant (CP-945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM. |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
CP 945598；Otenabant；CP945598
|
| 外观 |
Powder
|
| 可溶性/溶解性 |
10 mM in DMSO
|
| 生物活性 | |
| 靶点 |
Cannabinoid Receptor
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| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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.
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分子结构图
