生物活性 | |||
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描述 | Pioglitazone is a selective thiazolidinedione-based PPARγ agonist with EC50 value of 0.69μM for activating transcriptional activity of PPARγ and occupied PPARγ up to 90% at concentration of 100μM. Pioglitazone also showed weak activation effect on hPPARα[1][2]. Pioglitazone exhibited minimum effective dose at 300μM/kg for significant reduction in blood glucose in ob/ob mice[1]. Pioglitazone is used as an antidiabetic agent that improves hyperglycaemia and hyperlipidaemia in obese and diabetic animals through its action of reduction in hepatic and peripheral insulin resistance[2]. | ||
作用机制 | Pioglitazone exhibited competition binding to PPARγ as a high affinity ligand.[1] |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00861341 | - | Completed | - | - | |
NCT00719381 | Cystic Fibrosis | Phase 1 | Completed | - | United States, California ... 展开 >> University of Southern California Los Angeles, California, United States, 90089 收起 << |
NCT02733679 | Ataxia-Telangiectasia | Phase 4 | Completed | - | United Kingdom ... 展开 >> Ninewells Hospital Dundee, Angus, United Kingdom, DD19SY 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.81mL 0.56mL 0.28mL |
14.03mL 2.81mL 1.40mL |
28.06mL 5.61mL 2.81mL |
参考文献 |
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