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  • Tasimelteon

    • 他司美琼;BMS-214778;VEC-162
    货号: abs813161
    CAS号: 609799-22-6
    分子式: C15H19NO2
    分子量: 245.322
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs813161-5mg 1-2周 ¥460.00
    - +
    abs813161-10mg 1-2周 ¥828.00
    - +
    abs813161-50mg 1-2周 ¥2898.00
    - +
    abs813161-100mg 1-2周 ¥4671.00
    - +
    大包装询价
    产品描述
    描述

    Tasimelteon is a melatonin MT1 and MT2 receptor agonist.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    他司美琼;BMS-214778;VEC-162
    可溶性/溶解性
    DMSO ≥33 mg/mL
    生物活性
    靶点
    MT2 receptor ,MT1 receptor
    In vitro(体外研究)
    Tasimelteon is a circadian regulator that resets the master clock in the suprachiasmatic nuclei of the hypothalamus by binding to both melatonin MT1 and MT2 receptors making it a dual melatonin receptor agonist. The affinity of tasimelteon for the MT2 receptor is 4-fold higher than its affinity for the MT1 receptor.
    In vivo(体内研究)
    In rats and monkeys, the half-life of tasimelteon was approximately 2 h which is longer than the half-life of melatonin. Tasimelteon has a mean absolute bioavailability of approximately 38.3%. The higher oral-to-IV exposure ratios and decrease in the metabolite-to-parent ratios after IV administration for tasimelteon's metabolites indicate that although tasimelteon is subject to first-pass metabolism, a substantial fraction of its metabolism occurs post- rather than presystemically. Both oral and IV tasimelteon were well tolerated.
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