Dapagliflozin是口服活性的SGLT2抑制剂,可作用于2型糖尿病。
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
0.01-10 mg/kg (1 mL/kg) 口服处理
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] 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
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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