Pioglitazone
(Synonyms: 吡格列酮; U 72107) 目录号 : GC14948
Pioglitazone (PIO)是一种噻唑烷二酮类抗糖尿病药物,可作为PPARγ激动剂。它对人和小鼠PPARγ的EC50分别为0.93和0.99 µM..
Cas No.:111025-46-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
INS-1 cells |
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Preparation Method |
Cells were treated with pioglitazone (10 µM), with or without high glucose (30 mM). |
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Reaction Conditions |
10 µM;4h |
|
Applications |
Pioglitazone reversed the decrease in AMPK activity caused by high glucose in INS-1 cells. |
| Animal experiment [2]: | |
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Animal models |
ob/ob and adipo-/- ob/ob mice with a C57Bl/6 background |
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Preparation Method |
10-30 mg/kg pioglitazone or vehicle (0.25% carboxymethylcellulose) was adnimistered to mice by oral gavage once daily for 14 consecutive days. |
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Dosage form |
10-30 mg/kg; oral gavage; 14 days |
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Applications |
10 mg/kg pioglitazone can significantly improve insulin resistance and diabetes in ob/ob mice, and administration of 30 mg/kg pioglitazone has better effects. |
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References: [1]. Karunakaran U, Elumalai S, et,al. Pioglitazone-induced AMPK-Glutaminase-1 prevents high glucose-induced pancreatic β-cell dysfunction by glutathione antioxidant system. Redox Biol. 2021 Sep;45:102029. doi: 10.1016/j.redox.2021.102029. Epub 2021 Jun 3. PMID: 34107382; PMCID: PMC8187239. | |
Pioglitazone belongs to the class of glitazones or thiazolidinediones, a series of oral anti-diabetic drugs. Pioglitazone is a ligand for peroxisome proliferator-activated receptor γ (PPARγ) that acts as a PPARγ agonist with EC50 of 0.93 and 0.99 µM for human and mouse PPARγ[1-2].
Pioglitazone (10 µM;4h) reversed the decrease in AMPK activity caused by high glucose in INS-1 cells [3]. Pioglitazone (50 µM;48h) also inhibited tumor cell proliferation in the multicellular tumor spheroid culture system (MCTS) system[4].
Pioglitazone (oral,10 or 30 mg/kg once daily for 14 days) improves insulin resistance and diabetes[5].Four weeks of pioglitazone (10 or 20 mg/kg, daily, from 20- to 24-week-old) treatment alleviated the high-fat diet (HFD)-induced glucose-metabolic dysfunctions, upregulation of ventral hippocampal glial fibrillary acidic protein (GFAP), reduction of the total process lengths and the number of branch points of the ventral hippocampal CA1 GFAP-immunoreactive astrocytes and depressive phenotypes in mice[6]. Pioglitazone (oral gavage;10 mg/kg; once daily for 4 weeks) significantly reduced body weight (BW) myocardial hypertrophy glucose levels and improved associated dyslipidemia[7].
References:
[1]. Kuwabara K, Murakami K,et,al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose levels and modifies lipoprotein profiles in KK-Ay mice. J Pharmacol Exp Ther. 2004 Jun;309(3):970-7. doi: 10.1124/jpet.103.064659. Epub 2004 Feb 24. PMID: 14982965.
[2]. Legchenko E, Chouvarine P, et,al. PPARγ agonist pioglitazone reverses pulmonary hypertension and prevents right heart failure via fatty acid oxidation. Sci Transl Med. 2018 Apr 25;10(438):eaao0303. doi: 10.1126/scitranslmed.aao0303. PMID: 29695452.
[3]. Karunakaran U, Elumalai S, et,al. Pioglitazone-induced AMPK-Glutaminase-1 prevents high glucose-induced pancreatic β-cell dysfunction by glutathione antioxidant system. Redox Biol. 2021 Sep;45:102029. doi: 10.1016/j.redox.2021.102029. Epub 2021 Jun 3. PMID: 34107382; PMCID: PMC8187239.
[4]. Gottfried E, Rogenhofer S, et,al. Pioglitazone modulates tumor cell metabolism and proliferation in multicellular tumor spheroids. Cancer Chemother Pharmacol. 2011 Jan;67(1):117-26. doi: 10.1007/s00280-010-1294-0. Epub 2010 Mar 9. PMID: 20217088.
[5]. Kubota N, Terauchi Y, et,al. Pioglitazone ameliorates insulin resistance and diabetes by both adiponectin-dependent and -independent pathways. J Biol Chem. 2006 Mar 31;281(13):8748-55. doi: 10.1074/jbc.M505649200. Epub 2006 Jan 23. PMID: 16431926.
[6]. Lam YY, Tsai SF, et,al. Pioglitazone rescues high-fat diet-induced depression-like phenotypes and hippocampal astrocytic deficits in mice. Biomed Pharmacother. 2021 Aug;140:111734. doi: 10.1016/j.biopha.2021.111734. Epub 2021 May 19. PMID: 34022606.
[7]. Elrashidy RA, Asker ME, et,al. Pioglitazone attenuates cardiac fibrosis and hypertrophy in a rat model of diabetic nephropathy. J Cardiovasc Pharmacol Ther. 2012 Sep;17(3):324-33. doi: 10.1177/1074248411431581. Epub 2012 Jan 18. PMID: 22261714.
Pioglitazone属于格列酮类或噻唑烷二酮类,是一系列口服降糖药。Pioglitazone是过氧化物酶体增殖体激活受体γ (PPARγ)的配体,作为PPARγ激动剂,对人和小鼠PPARγ的EC50分别为0.93和0.99 µM [1-2]。
Pioglitazone (10 µM;4h)可逆转INS-1细胞高糖引起的AMPK活性下降[3]。Pioglitazone (50 µM;48h)在多细胞肿瘤球体培养系统(MCTS)中也能抑制肿瘤细胞的增殖[4]。
Pioglitazone (oral,10 or 30 mg/kg once daily for 14 days)改善胰岛素抵抗和糖尿病[5]。Pioglitazone (10 or 20 mg/kg, daily, from 20-24-week-old) 治疗4周可减轻小鼠HFD诱导的葡萄糖代谢功能障碍、海马腹侧GFAP上调、海马腹侧CA1 GFAP免疫反应星形胶质细胞总过程长度和分支点数量减少以及抑郁表型[6]。Pioglitazone (oral gavage;10 mg/kg;once daily for 4 weeks) 显著降低体重(BW)、心肌肥厚、血糖水平和改善相关的血脂异常[7]。
| Cas No. | 111025-46-8 | SDF | |
| 别名 | 吡格列酮; U 72107 | ||
| 化学名 | 5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3 | ||
| 分子式 | C19H20N2O3S | 分子量 | 356.44 |
| 溶解度 | ≥ 14.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL |
| 5 mM | 0.5611 mL | 2.8055 mL | 5.611 mL |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8055 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。