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  • Mirabegron
  • YM-178;米拉貝隆
  • 貨號: abs813340
    CAS號: 223673-61-8
    分子式: C21H24N4O2S
    分子量: 396.51
    產品說明書
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    貨號-規格 貨期 價格 數量
    abs813340-5mg 現貨 ¥2297.00
    - +
    abs813340-10mg 現貨 ¥3780.00
    - +
    abs813340-50mg 現貨 ¥9429.00
    - +
    ! 該貨號為 abs47025311 的新貨號。
    大包裝詢價
    產品描述
    描述

    Mirabegron是一種選擇性的beta3-adrenoceptor(β3腎上腺素受體)激動劑,EC50為22.4 nM。

    純度
    >98%
    儲存/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
    別名
    YM-178;米拉貝隆
    外觀
    淡黃色固體
    可溶性/溶解性
    Ethanol :8 mg/mL (20.17 mM)
    DMSO :73 mg/mL (184.1 mM)
    生物活性
    靶點
    Adrenergic Receptor
    In vitro(體外研究)
    Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR). EC50 value is 22.4 nM. EC50 values of Mirabegron for human β1- and β2-ARs are 10,000 nM or more, respectively. EC50 of Mirabegron in rat bladder strips precontracted with 10-6 M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10-7 M CCh is 0.78 μM. Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50 value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared by EC50 value, Mirabegron is approximately one third as potent as isoproterenol. The maximal relaxant effects of Mirabegron are 94±1%, that of CCh, indicating that Mirabegron acts a full agonist in the rat bladder. The maximal relaxant effects of Mirabegron is 89.4±2.3%.
    In vivo(體內研究)
    Mirabegron (YM178) produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. In contrast, Mirabegron does not decrease the amplitude of rhythmic bladder contraction at up to 3 mg/kg i.v.. On the contrary, Oxybutynin significantly increases the frequency of rhythmic bladder contraction and decreased its amplitude at doses of 0.272 mg/kg i.v. or more.
    參考文獻
    參考文獻
    Proarrhythmic safety of repeat doses of mirabegron in healthy subjects: a randomized, double-blind, placebo-, and active-controlled thorough QT study.
    Malik M, et al. Clin Pharmacol Ther. 2012 Dec;92(6):696-706. PMID: 23149929.
    Effects of mirabegron, a novel β3-adrenoceptor agonist, on primary bladder afferent activity and bladder microcontractions in rats compared with the effects of oxybutynin.
    Aizawa N, et al. Eur Urol. 2012 Dec;62(6):1165-73. PMID: 22981677.
    溫馨提示:本產品僅作科研實驗使用,不支持臨床等研究
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