Saxagliptin是选择性可逆的DPP4抑制剂,IC50和Ki分别为26 nM和1.3 nM。
Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
10 μmol/kg 口服
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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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