Otenabant (CP-945598) HCl

製品コードS8012 バッチS801201

印刷

化学情報

Chemical Structure Synonyms Otenabant Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H25Cl2N7O.HCl
分子量 546.88 CAS No. 686347-12-6
Solubility (25°C)* 体外 4-Methylpyridine (warmed with 50ºC water bath) 5 mg/mL (9.14 mM)
DMSO (warmed with 50ºC water bath) 1 mg/mL (1.82 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
0.5% methylcellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Otenabant (CP-945598) HCl 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. Phase 1.
in vitro CP-945598 HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. [1] CP-945598 HCl has low affinity with Ki of 7.6 μM for human CB2 receptors. [2]
in vivo CP-945598 HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. CP-945598 HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation. [1] CP-945598 also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. CP-945598 at 10 mg/kg promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. [2]

プロトコル(参考用のみ)

キナーゼアッセイ CB1 GTPγ [ 35S] Binding Assay
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: 100μg/mL bacitracin, 100μg/mL benzamidine, 5μg/mL aprotinin, 5μg/mL leupeptin. The assay mix is then incubated with increasing concentrations of antagonist (10-10 M to 10-5 M) for 10 min and challenged with the cannabinoid agonist CP-55,940 (10 μM). Assays are performed at 30 ℃ for 1 h. The FlashPlates are then centrifuged at 2000g for 10 min. Stimulation of GTPγ [35S] binding is then quantified using a Wallac Microbeta. EC50calculations are done using Prism by GraphPad. Inverse agonism is measured in the absence of agonist.
動物実験 動物モデル Sprague-Dawley rats
投薬量 ~30 mg/Kg
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Integrative discovery of treatments for high-risk neuroblastoma. [ Nat Commun, 2020, 11(1):71] PubMed: 31900415
E-cadherin-deficient cells have synthetic lethal vulnerabilities in plasma membrane organisation, dynamics and function [Godwin TD, et al. Gastric Cancer, 2018, 10.1007/s10120-018-0859-1] PubMed: 30066183

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。