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Dapagliflozin

达格列净,达格列嗪,BMS512148,BMS-512148,BMS 512148

Dapagliflozin是口服活性的SGLT2抑制剂,可作用于2型糖尿病。

目录号
EY0416
EY0416
EY0416
EY0416
纯度
99.21%
99.21%
99.21%
99.21%
规格
5 mg
10 mg
50 mg
100 mg
原价
720
990
2520
4250
售价
720
990
2520
4250
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

    Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    0.01-10 mg/kg (1 mL/kg) 口服处理

  • 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] Meng W, et al. J Med Chem, 2008, 51(5), 1145-1149.

    分子式
    C21H25ClO6
    分子量
    408.87
    CAS号
    461432-26-8
    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
    30 mg/mL

    体内溶解度

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

    NCT01156246 Healthy Drug: Dapagliflozin/Metformin AstraZeneca|Bristol-Myers Squibb Phase 1 2010-06-01 2012-05-31
    NCT03030235 Chronic Heart Failure With Preserved Systolic Function Drug: Dapagliflozin 10Mg Oral Tablet|Drug: Dapagliflozin matching placebo Saint Luke's Health System Phase 4 2017-03-01 2017-03-01
    NCT02585804 Focal Segmental Glomerulosclerosis Drug: Dapagliflozin University Health Network, Toronto|AstraZeneca|University of Toronto|Toronto General Hospital Phase 4 2015-09-01 2015-10-22
    NCT02973477 Type2 Diabetes|Cardiovascular Diseases Drug: Dapagliflozin|Drug: Glimepiride University of Michigan|AstraZeneca Phase 4 2017-01-12 2017-02-14
    NCT02426541 Type 2 Diabetes Mellitus Drug: Dapagliflozin|Drug: Placebo AstraZeneca|Antaros Medical AB|Bioventure Hub|43183 M枚lndal|Sweden Phase 4 2015-03-01 2016-05-11
    NCT02653482 Chronic Heart Failure With Reduced Systolic Function Drug: Dapagliflozin|Drug: Dapagliflozin matching placebo Saint Luke's Health System Phase 4 2016-03-01 2017-03-01
    NCT02777073 Type 1 Diabetes Drug: Farxiga|Drug: Victoza|Drug: Placebo University at Buffalo Phase 3 2016-03-01 2017-02-08
    NCT02371187 Physical Activity Drug: Dapagliflozin|Drug: Placebo Christopher Bell|AstraZeneca|Colorado State University Phase 2 2015-06-01 2017-02-16
    NCT02608905 Type 2 Diabetes Mellitus Drug: Dapagliflozin|Drug: Placebo Baylor College of Medicine Phase 4 2015-11-01 2016-11-30
    NCT02211742 Fasting Glucose|Glucose Excursion|Glycemic Control Drug: Dapagliflozin Medical University Innsbruck|Medical University of Graz|University of Bern Phase 4 2014-08-01 2015-04-07
    NCT02919345 Diabetes Mellitus, Type 2|Coronary Artery Disease|Carotid Artery Diseases Drug: Dapagliflozin 10 mg|Drug: Glibenclamide 5 mg University of Campinas, Brazil|AstraZeneca Phase 4 2017-01-01 2016-09-28
    NCT01195662 Type 2 Diabetes Drug: Dapagliflozin|Drug: Placebo matching Dapagliflozin AstraZeneca|Bristol-Myers Squibb Phase 3 2010-10-01 2016-11-10
    NCT02413398 Type 2 Diabetes Mellitus Drug: Dapagliflozin 10 mg|Drug: Matching Placebo for Dapagliflozin AstraZeneca Phase 3 2015-06-15 2017-03-22
    NCT02577159 Diabetes Mellitus, Type 2 Drug: Dapagliflozin Osaka University Phase 4 2015-07-01 2016-09-28
    NCT02887677 Diabetes Mellitus Drug: Dapagliflozin|Drug: Placebo Hellenic Society for Medical Education Phase 4 2016-10-01 2016-08-29
    NCT03036150 Chronic Kidney Disease Drug: Dapagliflozin|Drug: Placebo AstraZeneca Phase 3 2017-02-01 2017-02-09
    NCT02372955 Diabetes Mellitus Type 2 Drug: dapagliflozin|Drug: glimpiride Gulf Regional Research & Educational Services, LLC Phase 4 2015-02-01 2015-02-20
    NCT03036124 Chronic Heart Failure With Reduced Ejection Fraction (HFrEF) Drug: Dapagliflozin|Drug: Placebo AstraZeneca Phase 3 2017-02-01 2017-02-17
    NCT02919059 Diabetes Mellitus, Type 2 Drug: Dapagliflozin 10 mg|Drug: Glimepiride 4 mg IInstituto Gallego de Medicina Vascular Phase 4 2016-10-01 2016-09-27
    NCT02981966 Diabetes Mellitus, Type 2 Drug: Dapagliflozin|Drug: Placebo The University of Texas Health Science Center at San Antonio|AstraZeneca Phase 4 2017-01-01 2016-12-02

    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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