Anamorelin

製品コードS4980 バッチS498003

印刷

化学情報

Chemical Structure Synonyms ONO-7643, RC-1291, ST-1291 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C31H42N6O3
分子量 546.70 CAS No. 249921-19-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (182.91 mM)
Ethanol 100 mg/mL (182.91 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
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (9.15mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.410mg/ml (0.75mM) Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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 Anamorelin (ONO-7643, RC-1291, ST-1291) is an orally active, high-affinity, selective agonist of the ghrelin receptor with an EC50 value of 0.74 nM in the HEK293/GRLN FLIPR assay.
in vitro Anamorelin shows significant agonist and binding activity on the ghrelin receptor, and stimulates growth hormone (GH) release in vitro. Through its ghrelin and GH-releasing activity, this compound has both orexigenic and anabolic properties. In the screening for its activity, 10 μM of this chemical shows weak binding to the calcium channel L-type receptors, the serotonin transporter, and the sodium channel. Therefore, it exhibits a high selectivity versus ghrelin receptors[2]. By inhibiting nuclear factor κB, this agent reduces production of pro-inflammatory cytokines and stops muscle breakdown (inhibits proteolysis)[3].
in vivo In rats, Anamorelin significantly and dose-dependently increases food intake and body weight at all dose levels compared with control, and significantly increased growth hormone (GH) levels at 10 or 30 mg/kg doses. Growth hormone and IGF-1 levels increase following this compound administration in pigs. It is orally active and has a longer half-life (approximately 7 h) than ghrelin. It stimulates neuroendocrine responses and can induce rapid positive effects on appetite and metabolism[2]. Plasma clearance of radiolabelled anamorelin shows that most of the drug is excreted in the feces (92%). Food decreases the area under the curve (AUC) of this chemical by 4-fold. Metabolism occurs by CYP3A4. In mouse tumor models, such as Lewis lung and human bronchioalveolar carcinoma, it does not promote tumor growth[3].

プロトコル(参考用のみ)

動物実験 動物モデル A549 NSCLC xenografts
投薬量 3, 10, or 30 mg/kg
投与方法 p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/23579947/
  • https://pubmed.ncbi.nlm.nih.gov/25267366/

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：

High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction [ Drug Test Anal, 2020, 10.1002/dta.2917] PubMed: 32852861

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。