Pioglitazone (U 72107) 是一种具有口服活性的选择性PPARγ(peroxisome proliferator-activated receptor) 激动剂，高亲和力结合到 PPARγ 配体结合域，作用于人和鼠 PPARγ 的EC50分别为 0.93 和 0.99 μM。Pioglitazone 可用于糖尿病研究。
| 生物活性 | Pioglitazone (U 72107) is an orally active and selectivePPARγ(peroxisome proliferator-activated receptor) agonist with high affinity binding to thePPARγligand-binding domain withEC50of 0.93 and 0.99 μM for human and mousePPARγ, respectively. Pioglitazone can be used in diabetes research[2][3][4]. |
| IC50& Target[1] | hPPARγ 0.93 μM (EC50) | mouse PPARγ 0.99 μM (EC50) | hPPARδ 43 μM (EC50) | hPPARα 100 μM (EC50) | mouse PPARα 100 μM (EC50) |
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体外研究
(In Vitro) | Pioglitazone (0.5 or 1 μM, 5 days) can completely prevent AGEs (advanced glycation end-products)-induced β-cell necrosis and the increase of caspase-3 thereby avoiding the impaired viability caused by AGEs in pancreatic beta cell line HIT-T15[2].
Pioglitazone (1 μM, 1 h) can stimulate insulin secretion induced by low glucose concentration and attenuate the GSSG/GSH ratio in cells cultured with AGEs[2].
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体内研究
(In Vivo) | Pioglitazone (oral gavage, 10 or 30 mg/kg, once daily, 14 days) can induce improvements in insulin resistance and diabetes that may be lipocalin-dependent in the liver but not in skeletal muscle[3].
Pioglitazone (oral gavage, 10 mg/kg, once daily, 4 weeks) can significantly reduce body weight (BW), cardiac hypertrophy, elevated blood glucose levels and improve the associated dyslipidemia[4].
| Animal Model: | ob/ob andadipo-/-ob/ob mice with a C57Bl/6 background[3] | | Dosage: | 10 or 30 mg/kg | | Administration: | Oral gavage; once daily; 14 days | | Result: | Showed no changes of serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob andadipo-/-ob/ob C57BL/6 mice at 10 mg/kg but significantly reduced to a similar degree at 30 mg/kg.
Also showed no changes of expressions of TNFα and resistin in adipose tissues of ob/ob andadipo-/-ob/ob mice at 10 mg/kg but decreased at 30 mg/kg. |
| Animal Model: | Male Wistar albino rats[4] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; once daily; 4 weeks | | Result: | Decreased the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB), TGF-β1 gene expression and regulated the expression of MMP-2/TIMP-2 system. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 40 mg/mL(112.22 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL | | 5 mM | 0.5611 mL | 2.8055 mL | 5.6110 mL | | 10 mM | 0.2806 mL | 1.4028 mL | 2.8055 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 0.5%CMC-Na/saline water Solubility: 10 mg/mL (28.06 mM); Suspened solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (5.84 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.84 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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