货号:A612927
同义名:
匹格列酮
/ U 72107; AD-4833
Pioglitazone is an agonist of peroxisome proliferator-activated receptor gamma (PPARγ, EC50 = 500-600 nM) over PPAR⍺. It also a thiazolidinedione (TZD) anti-diabetic.
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产品名称 | PPARα ↓ ↑ | PPARβ/δ ↓ ↑ | PPARγ ↓ ↑ | PPARδ ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Fenofibric acid | ✔ | 98% | |||||||||||||||||
GW6471 |
++
PPARα, IC50: 0.24 μM |
99%+ | |||||||||||||||||
GSK3787 |
++
PPARδ, pIC50: 6.6 |
++
PPARδ, pIC50: 6.6 |
99%+ | ||||||||||||||||
FH535 | ✔ | 98%+ | |||||||||||||||||
GW9662 |
+++
PPARα, IC50: 32 nM |
+++
PPARγ, IC50: 3.3 nM |
98% | ||||||||||||||||
T0070907 |
++++
PPARγ, IC50: 1 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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] |
Dose | Rat: 20 mg/kg[3] (p.o.) Mice: 1 mg/kg - 30 mg/kg[4] (p.o.) | |||||||||||||||||||||||||||||||||||||||||||||
Administration | p.o. | |||||||||||||||||||||||||||||||||||||||||||||
Pharmacokinetics |
|
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 << |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 111025-46-8 |
分子式 | C19H20N2O3S |
分子量 | 356.44 |
SMILES Code | O=C(N1)SC(CC2=CC=C(OCCC3=NC=C(CC)C=C3)C=C2)C1=O |
MDL No. | MFCD00865504 |
别名 | 匹格列酮 ;U 72107; AD-4833 |
运输 | 蓝冰 |
InChI Key | HYAFETHFCAUJAY-UHFFFAOYSA-N |
Pubchem ID | 4829 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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