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Saxagliptin

沙克列汀,BMS-477118,BMS 477118,BMS477118

Saxagliptin是选择性可逆的DPP4抑制剂,IC50和Ki分别为26 nM和1.3 nM。

目录号
EY1430
EY1430
EY1430
EY1430
纯度
99.14%
99.14%
99.14%
99.14%
规格
1 mg
5 mg
10 mg
50 mg
原价
240
480
730
2100
售价
240
480
730
2100
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

    Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    10 μmol/kg 口服

  • 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] Tahrani AA, et al. Adv Ther. 2009, 26(3), 249-262.

    分子式
    C18H25N3O2
    分子量
    315.41
    CAS号
    361442-04-8
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    62 mg/mL
    Water
    62 mg/mL
    Ethanol
    25 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
    NCT02307695 Type 1 Diabetes Drug: Saxagliptin|Drug: Insulin Nanjing Medical University Phase 4 2014-11-01 2016-07-05
    NCT00935467 Type 2 Diabetes Mellitus Drug: Saxagliptin AstraZeneca Phase 1 2009-07-01 2015-05-04
    NCT01552018 Coronary Artery Disease|Diabetes Mellitus Type 2 Drug: Saxagliptin|Drug: Placebo Oslo University Hospital Phase 4 2012-03-01 2014-06-17
    NCT00770302 Type 2 Diabetes Drug: Saxagliptin AstraZeneca|Bristol-Myers Squibb Phase 1 2008-10-01 2009-07-08
    NCT01548651 Impaired Glucose Tolerance Drug: Saxagliptin|Drug: Placebo Baylor College of Medicine Phase 4 2012-02-01 2016-11-30
    NCT02243176 Type 2 Diabetes Mellitus Drug: Saxagliptin|Drug: Acarbose AstraZeneca Phase 4 2014-09-01 2016-01-11
    NCT01441869 Bioequivalence, Log-transformed AUCss and Cmax,ss Values for Saxagliptin and Metformin Drug: Onglyza (saxagliptin)|Drug: Diabex|Drug: 5-mg saxagliptin/1000 mg metformin|Drug: Diabex|Drug: 5-mg saxagliptin/500 mg metformin AstraZeneca Phase 1 2011-10-01 2012-02-07
    NCT02462369 Microalbuminuria|Microalbuminuria /Creatinine Ratios ACR Drug: Saxagliptin|Drug: glimepiride The Second Hospital of Nanjing Medical University Phase 4 2015-06-01 2015-07-27
    NCT02407899 Diabetes Mellitus, Type 1 Drug: Saxagliptin|Drug: Vitamin D3|Drug: Insulin Second Xiangya Hospital of Central South University|National Clinical Research Center for Metabolic Diseases, China Phase 4 2015-03-01 2015-11-17
    NCT01765270 Type 2 Diabetes Mellitus|Cardiovascular Disease Drug: Saxagliptin|Drug: Placebo Duke University Phase 4 2013-03-01 2015-05-07
    NCT02280486 Type 2 Diabetes Drug: Saxagliptin|Drug: Glimepiride The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School|The First Affiliated Hospital with Nanjing Medical University|Zhongda Hospital|Nanjing PLA General Hospital|Changzhou No.2 People's Hospital|The First Affiliated Hospital of Soochow University|Wuxi People's Hospital|The First Affiliated Hospital of Anhui Medical University|Huan'an First People's Hospital Phase 4 2015-01-01 2016-10-31
    NCT01319357 Diabetes Mellitus Type 2 Drug: Saxagliptin|Drug: Placebo University of Erlangen-Nrnberg Medical School Phase 3 2010-10-01 2014-02-11
    NCT01521312 Impaired Glucose Tolerance Drug: saxagliptin|Other: placebo pill Assistance Publique - Hpitaux de Paris Phase 2 2012-09-01 2015-02-02
    NCT01068743 Type 2 Diabetes Mellitus Drug: saxagliptin|Drug: metformin|Drug: saxagliptin + metformin (FDC tablet) AstraZeneca Phase 1 2010-02-01 2015-04-21
    NCT02377388 Platelet Aggregation During Acute Myocardial Infarction Drug: saxagliptin|Drug: placebo University of Sao Paulo General Hospital|InCor Heart Institute Phase 3 2017-02-07 2017-02-20
    NCT02104804 Type 2 Diabetes Mellitus Drug: Saxagliptin 5mg|Drug: Placebo for Saxagliptin AstraZeneca Phase 3 2014-05-01 2016-06-14
    NCT02182895 Diabetes Mellitus Drug: Saxagliptin Brigham and Women's Hospital Phase 4 2014-07-01 2016-02-08
    NCT02024477 Type 2 Diabetes Drug: Saxagliptin|Drug: Placebo George Washington University|AstraZeneca Phase 4 2013-11-01 2017-03-17
    NCT01552005 Type 2 Diabetes Mellitus (T2D) Drug: Saxagliptin AstraZeneca 2012-05-01 2016-06-06
    NCT00757588 Type 2 Diabetes Drug: Saxagliptin, 5 mg + insulin|Drug: Placebo + insulin AstraZeneca Phase 3 2008-11-01 2015-05-08
    NCT01192152 Diabetes Mellitus Drug: saxagliptin|Drug: Glucophage XR|Drug: saxagliptin + metformin XR (FDC tablet) AstraZeneca Phase 1 2009-11-01 2015-04-22
    NCT01192139 Diabetes Mellitus Drug: saxagliptin|Drug: metformin XR|Drug: saxagliptin + metformin XR (FDC tablet) AstraZeneca Phase 1 2009-11-01 2015-05-04
    NCT01305551 Type 2 Diabetes Drug: Saxagliptin|Drug: Metformin XR|Drug: Saxagliptin/Metformin XR FDC AstraZeneca Phase 1 2011-03-01 2014-06-04
    NCT02285985 Type 2 Diabetes Mellitus (T2DM) Drug: Saxagliptin|Drug: Placebo Phoenix VA Health Care System|Bristol-Myers Squibb Phase 4 2013-02-01 2017-01-31
    NCT02304081 Type2 Diabetes Mellitus Drug: Saxagliptin|Drug: Placebo for Saxagliptin Prof. Dr. Thomas Forst|Profil Mainz GmbH & Co KG Phase 4 2015-01-01 2016-09-26

    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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