1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. Otenabant Hydrochloride

Otenabant Hydrochloride  (Synonyms: CP 945598 Hydrochloride)

目录号: HY-10871A
产品使用指南

Otenabant (CP945598)盐酸盐是CB1受体高亲和性拮抗剂,Ki为0.7 nM。

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Otenabant Hydrochloride Chemical Structure

Otenabant Hydrochloride Chemical Structure

CAS No. : 686347-12-6

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Otenabant Hydrochloride 的其他形式现货产品:

Other Forms of Otenabant Hydrochloride:

查看 Cannabinoid Receptor 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Otenabant Hydrochloride is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

IC50 & Target

Ki: 0.7 nM (CB1)

体外研究
(In Vitro)

Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors[1]. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[1]. 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

546.88

Formula

C25H26Cl3N7O

CAS 号
中文名称

奥替那班盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Kinase Assay
[2]

Membranes are prepared from CHOK1 cells stably transfected with the human CB-1 receptor cDNA. GTPγ [35S] binding assays are performed in a 96-well FlashPlate format in duplicate using 100 pM GTPγ [35S] and 10μg membrane per well in assay buffer composed of 50 mM Tris HCl, pH 7.4, 3 mM MgCl2, pH 7.4, 10 mM MgCl2, 20 mM EGTA, 100 mM NaCl, 30 µM GDP, 0.1% bovine serum albumin, and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The assay mix is then incubated with increasing concentrations of antagonist (10-10M to 10-5 M) for 10 min and challenged with the cannabinoid agonist CP-55,940 (10 μM). Assays are performed at 30°C for 1 h. The FlashPlates are then centrifuged at 2000 g for 10 min. Stimulation of GTPγ [35S] binding is then quantified using a Wallac Microbeta. EC50 calculations are done using Prism by GraphPad. Inverse agonism is measured in the absence of agonist.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Male, 14 week old C57/Bl6/6J mice which has been maintained on a high fat diet (45% kcal from fat) for 6 weeks are selected for the DIO weight loss study. The animals body weights range at least five standard deviations from age-matched chow-fed control animals mean body weight. Mice are singly housed. The mean starting weight of all animals is 38.9±0.5 g. On day 0, mice are randomLy assigned to treatment groups (n=10 per group). Mice are dosed daily with vehicle or 10 mg/kg (p.o.) CP-945,598 over 10 days, starting approximately at 30 min before the start of the 12 h dark cycle. BW and food intake are recorded daily. Analysis of variance and comparison of means are calculated for daily and cumulative FI and cumulative BW measurements. P < 0.05 is considered statistically significant.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Otenabant Hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Otenabant Hydrochloride
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HY-10871A
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