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Synonyms | ONO-7643, RC-1291, ST-1291 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C31H42N6O3 |
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分子量 | 546.70 | CAS No. | 249921-19-5 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (182.91 mM) | |
Ethanol | 50 mg/mL (91.45 mM) | |||
Water | Insoluble | |||
* <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. |
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. |
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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, anamorelin has both orexigenic and anabolic properties. In the screening for anamorelin activity, 10 μM Anamorelin 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, anamorelin 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 anamorelin administration in pigs. Anamorelin 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 anamorelin by 4-fold. Metabolism occurs by CYP3A4. In mouse tumor models, such as Lewis lung and human bronchioalveolar carcinoma, anamorelin does not promote tumor growth[3]. |
動物実験 | 動物モデル | A549 NSCLC xenografts |
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投薬量 | 3, 10, or 30 mg/kg | |
投与方法 | p.o. |
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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。