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  • Anamorelin HCl
    • RC-1291 hydrochloride; ONO-7643 hydrochloride; RC1291 hydrochloride; ONO7643 hydrochloride; RC 1291 hydrochloride; ONO 7643 hydrochloride
    货号: abs811142
    CAS号: 861998-00-7
    分子式: C31H43ClN6O3
    分子量: 583.16
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs811142-5mg 1-2周 ¥1213.00
    - +
    abs811142-10mg 1-2周 ¥1820.00
    - +
    abs811142-50mg 1-2周 ¥5943.00
    - +
    大包装询价
    产品描述
    描述

    Anamorelin is currently 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 hydrochloride; ONO-7643 hydrochloride; RC1291 hydrochloride; ONO7643 hydrochloride; RC 1291 hydrochloride; ONO 7643 hydrochloride
    可溶性/溶解性
    DMSO: ≥ 28 mg/mL
    生物活性
    靶点
    GHSR
    In vitro(体外研究)
    In the FLIPR assay, Anamorelin (ANAM) shows significant agonist activity on the ghrelin receptor, with EC50 value of 0.74 nM. No significant antagonist activity is observed with Anamorelin at concentrations of up to 1,000 nM. In the binding experiments, Anamorelin binds to the ghrelin receptor with a binding affinity constant (Ki) of 0.70 nM. In the competition assay with radiolabeled ibutamoren (35S-MK-677; another ghrelin receptor agonist) Anamorelin (ANAM) is also found to bind with high affinity to the ghrelin receptor (IC50=0.69 nM). In rat pituitary cells incubated with Anamorelin, there is a dose-dependent stimulatory effect on GH release and the potency (EC50) is 1.5 nM. Anamorelin is screened for activity against a set of over 100 receptors, ion channels, transporters, and enzymes. Anamorelin demonstrates binding to the tachykinin neurokinin 2 (NK2) site (IC50=0.021 μM); however, a subsequent NK2 functional assay demonstrates no functional activity.
    In vivo(体内研究)
    In rats, Anamorelin (ANAM) at an oral dose of 3, 10, or 30 mg/kg once daily significantly increases both food intake and body weight from Day 2 to Day 7 of treatment compared with the vehicle control. The cumulative change in food intake and weight gain increases dose-dependently, and these changes are significant at all dose levels (P0-6h in rats.
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