Mirabegron

米拉贝隆,YM 178,YM178,YM-178

Mirabegron(YM178)是β3肾上腺素受体激动剂,EC50为22.4 nM。

目录号
EY0885
EY0885
EY0885
EY0885
纯度
99.64%
99.64%
99.64%
99.64%
规格
1 mg
5 mg
10 mg
50 mg
原价
335
760
1200
4300
售价
335
760
1200
4300
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Takasu T, et al. J Pharmacol Exp Ther, 2007, 321(2), 642-647.
    [2] Krauwinkel W, van Dijk J, Schaddelee M et al. Pharmacokinetic Properties of Mirabegron, a β(3)-Adrenoceptor Agonist: Results From Two Phase I, Randomized, Multiple-Dose Studies in Healthy Young and Elderly Men and Women. Clin Ther. 2012 Oct;34(10):2144-60.
    [3] Tyagi P, Tyagi V, Chancellor M. Mirabegron: a safety review. Expert Opin Drug Saf. 2011 Mar;10(2):287-94.

    分子式
    C21H24N4O2S
    分子量
    396.51
    CAS号
    223673-61-8
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    82 mg/mL
    Water
    <1 mg/mL
    Ethanol
    10 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00940121 Healthy|Pharmacokinetics of Mirabegron Drug: mirabegron|Drug: mirabegron Astellas Pharma Inc Phase 1 2009-04-01 2013-07-01
    NCT00939757 Healthy|Pharmacokinetics of Mirabegron Drug: mirabegron Astellas Pharma Inc Phase 1 2009-05-01 2013-06-24
    NCT00776516 Pharmacokinetics of YM178 Drug: mirabegron|Drug: rifampin Astellas Pharma Inc Phase 1 2008-10-01 2013-07-01
    NCT01478568 Pharmacokinetics of Mirabegron|Healthy Subjects Drug: mirabegron|Drug: desipramine Astellas Pharma Inc Phase 1 2008-10-01 2014-04-08
    NCT01747564 Healthy Subjects|Plasma Concentration of Mirabegron Drug: YM178 (mirabegron) Astellas Pharma Inc Phase 1 2012-08-01 2012-12-10
    NCT02211846 Pharmacokinetics of Mirabegron|Neurogenic Detrusor Overactivity|Overactive Bladder Drug: Mirabegron Astellas Pharma Inc|Astellas Pharma Europe B.V. Phase 1 2014-07-01 2015-10-02
    NCT01478529 Pharmacokinetics of Mirabegron|Bioavailability|Healthy Subjects Drug: mirabegron OCAS|Drug: mirabegron Astellas Pharma Inc Phase 1 2006-02-01 2013-06-25
    NCT02495389 Overactive Bladder Drug: mirabegron Loyola University|Astellas Pharma US, Inc. Phase 4 2015-01-01 2017-03-09
    NCT02916693 Erectile Dysfunction|Overactive Bladder|Urinary Incontinence Drug: Mirabegron Johns Hopkins University|Astellas Pharma US, Inc. Phase 1|Phase 2 2016-09-01 2016-09-23
    NCT01285596 Healthy Volunteers|Pharmacokinetics of Mirabegron Drug: Mirabegron Astellas Pharma Inc Phase 1 2009-03-01 2013-07-01
    NCT02981459 Urinary Frequency/Urgency|Bladder Irritable|Bladder Pain Syndrome Drug: Mirabegron State University of New York at Buffalo|Astellas Pharma Inc Phase 4 2017-01-01 2016-12-02
    NCT01478490 Pharmacokinetics of Mirabegron|Healthy Subjects Drug: mirabegron|Drug: metoprolol Astellas Pharma Inc Phase 1 2002-09-01 2014-04-08
    NCT01297192 Healthy Volunteers|Pharmacokinetics of Mirabegron Drug: solifenacin succinate|Drug: mirabegron Astellas Pharma Inc Phase 1 2009-03-01 2013-07-25
    NCT02044510 Urinary Bladder, Neurogenic Drug: Mirabegron|Drug: Placebo Lawson Health Research Institute Phase 2|Phase 3 2014-07-01 2017-03-21
    NCT01284868 Healthy Volunteers|Pharmacodynamics of Mirabegron Drug: mirabegron|Drug: Bisoprolol|Drug: propranolol|Drug: placebo Astellas Pharma Inc Phase 1 2009-07-01 2013-07-01
    NCT02570035 Overactive Bladder|Cardiovascular Disease Drug: Mirabegron Astellas Pharma Inc 2012-12-01 2015-10-06
    NCT02751931 Neurogenic Detrusor Overactivity Drug: Mirabegron Astellas Pharma Europe B.V.|Astellas Pharma Inc Phase 3 2016-06-01 2016-12-27
    NCT01334905 Healthy Volunteer|Pharmacokinetics of YM178 Drug: YM178 Astellas Pharma Inc|Astellas Pharma Taiwan, Inc. Phase 1 2011-03-01 2013-06-10
    NCT00965926 Healthy Volunteer|Pharmacokinetics of YM178 Drug: YM178 Astellas Pharma Inc Phase 1 2009-07-01 2013-07-15
    NCT01964183 Pharmacokinetics of Mirabegron and Tolterodine|Healthy Drug: tolterodine|Drug: mirabegron Astellas Pharma Inc Phase 4 2013-06-01 2013-10-15
    NCT00912964 Urinary Bladder, Overactive Drug: Mirabegron|Drug: Placebo Astellas Pharma Inc Phase 3 2009-04-01 2015-06-05
    NCT02536976 Parkinson Disease|Overactive Bladder|Impaired Cognition Drug: mirabegron|Drug: Placebo HealthPartners Institute Phase 4 2015-12-01 2016-10-25

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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