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  • Opicapone (BIA 9-1067)

    • BIA9-1067
    货号: abs811274
    CAS号: 923287-50-7
    分子式: C15H10Cl2N4O6
    分子量: 413.17
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    货号-规格 货期 价格 数量
    abs811274-5mg 4周 ¥2668.00
    - +
    abs811274-10mg 4周 ¥4608.00
    - +
    abs811274-50mg 4周 ¥14553.00
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    大包装询价
    产品描述
    描述

    opicapone is a novel catechol-O-methyltransferase inhibitor

    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
    BIA9-1067
    可溶性/溶解性
    10 mM in DMSO
    生物活性
    靶点
    COMT
    In vitro(体外研究)
    Opicapone has a prolonged inhibitory effect on peripheral COMT, which extends the bioavailability of levodopa, without inducing toxicity. Opicapone decreases the ATP content of the cells with IC50 values of 98 μM. Incubation of human primary hepatocytes for 24 h with increasing concentrations of Tolcapone, entacapone or Opicapone resulted in a concentration-dependent decrease in the mitochondrial membrane potential of the cells, evaluated by the ratio JC-1 aggregates over JC-1 monomer (ratio λex 544 λem 590 over λex 485 λem 538). Opicapone decreases the mitochondrial membrane potential of the cells with IC50 of 181 μM.
    In vivo(体内研究)
    Opicapone inhibits rat peripheral COMT with ED50 values below 1.4 mg/kg up to 6 h post-administration. The effect is sustained over the first 8 h and by 24 h COMT had not returned to control values. A single administration of Opicapone resulted in increased and sustained plasma levodopa levels with a concomitant reduction in 3-O-methyldopa from 2 h up to 24 h post-administration, while Tolcapone produced significant effects only at 2 h post-administration. The effects of Opicapone on brain catecholamines after levodopa administration are sustained up to 24 h post-administration. Opicapone is also the least potent compound in decreasing both the mitochondrial membrane potential and the ATP content in human primary hepatocytes after a 24 h incubation period.
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