Pioglitazone

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Chemical Structure| 111025-46-8 同义名 : 匹格列酮 ;U 72107; AD-4833
CAS号 : 111025-46-8
货号 : A612927
分子式 : C19H20N2O3S
纯度 : 99% (HPLC)
分子量 : 356.44
MDL号 : MFCD00865504
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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
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

[1]Willson TM, Cobb JE, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8.

[2]Sakamoto J, Kimura H, et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem Biophys Res Commun. 2000 Nov 30;278(3):704-11.

[3]Ding SY, Shen ZF, et al. Pioglitazone can ameliorate insulin resistance in low-dose streptozotocin and high sucrose-fat diet induced obese rats. Acta Pharmacol Sin. 2005 May;26(5):575-80.

[4]Ahn HY, Kim HH, et al. Effects of Pioglitazone on Nonalcoholic Fatty Liver Disease in the Absence of Constitutive Androstane Receptor Expression. PPAR Res. 2018 Sep 27;2018:9568269.

[5]AD 4833