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  • Anamorelin
    • RC-1291; ONO-7643; RC1291; ONO7643; RC 1291; ONO 7643
    货号: abs810786
    CAS号: 249921-19-5
    分子式: C31H42N6O3
    分子量: 546.7
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810786-5mg 1-2周 ¥761.00
    - +
    abs810786-10mg 1-2周 ¥964.00
    - +
    abs810786-50mg 1-2周 ¥5292.00
    - +
    abs810786-100mg 1-2周 ¥6946.00
    - +
    大包装询价
    产品描述
    描述
    Anamorelin(RC1291; ONO-7643) is a synthetic orally active ghrelin receptor agonist which is under development for the management of non-small lung cancer associated cachexia/anorexia.
    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    RC-1291; ONO-7643; RC1291; ONO7643; RC 1291; ONO 7643
    外观
    Powder
    可溶性/溶解性
    10 mM in DMSO
    生物活性
    靶点
    ghrelin receptor
    In vitro(体外研究)
    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. By inhibiting nuclear factor κB, anamorelin reduces production of pro-inflammatory cytokines and stops muscle breakdown (inhibits proteolysis).
    In vivo(体内研究)
    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. 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.
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