Rosiglitazone
(Synonyms: 罗格列酮; BRL 49653) 目录号 : GC16444
A PPARγ agonist
Cas No.:122320-73-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Non–small cell lung carcinoma (NSCLC) cells (H1792 and H1838) |
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Preparation method |
The solubility of this compound in DMSO is >17.9 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10 μmol/L, 48 hours |
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Applications |
Rosiglitazone reduced the phosphorylation of Akt and increased phosphatase and tensin homologue (PTEN) protein expression in non–small cell lung carcinoma (NSCLC) cells (H1792 and H1838), and this was associated with inhibition of NSCLC cell proliferation. Rosiglitazone increased the phosphorylation of AMP-activated protein kinase α (AMPKα), a downstream kinase target for LKB1, whereas it decreased phosphorylation of p70 ribosomal protein S6 kinase (p70S6K), a downstream target of mammalian target of rapamycin (mTOR). |
| Animal experiment [2]: | |
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Animal models |
C57/BL6 mice |
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Dosage form |
8 mg/kg per day |
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Application |
In C57/BL6 mice underwent femoral angioplasty, treatment with rosiglitazone (8 mg/kg per day) attenuated neointimal formation. In a BM transplantation model, Rosiglitazone caused a 6-fold increase in colony formation by human endothelial progenitor cells, promoted the differentiation of APCs toward the endothelial lineage in mouse BM in vivo and in human peripheral blood in vitro, and inhibited the differentiation toward the smooth muscle cell lineage. Within the neointima, rosiglitazone stimulated APCs to differentiate into mature endothelial cells and caused earlier reendothelialization. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Han S W, Roman J. Rosiglitazone suppresses human lung carcinoma cell growth through PPARγ-dependent and PPARγ-independent signal pathways[J]. Molecular cancer therapeutics, 2006, 5(2): 430-437. [2]. Wang C H, Ciliberti N, Li S H, et al. Rosiglitazone facilitates angiogenic progenitor cell differentiation toward endothelial lineage[J]. Circulation, 2004, 109(11): 1392-1400. |
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Rosiglitazone is a potent agonist of peroxisome proliferator-activated receptor γ (PPARγ), a subfamily of the nuclear-receptor superfamily which is predominately expressed in adipose tissue and regulates gene expression responding to ligand binding. Belonging to the thiazolidinedione (TZD) class, rosiglitazone, like other TZD members, binds to PPARγ DNA as heterodimers and activate transcription of various metabolic regulators involved in the differentiation of stem cells into adipocytes and increased expression of genes regulating the metabolism of glucose and lipid. Rosiglitazone is used to treat patients with type II diabetes mellitus for its strong ability to improve insulin sensitization through its effects either on fatty acid uptake and storage in adipose tissue or on adiokines.
罗格列酮是过氧化物酶体增殖物激活受体γ（PPARγ）的强效激动剂，PPARγ是核受体超家族的一个亚家族，主要在脂肪组织中表达，并调节对配体结合的基因表达。罗格列酮属于噻唑烷二酮（TZD）类，与其他TZD成员一样，作为异二聚体与PPARγDNA结合，激活参与干细胞分化为脂肪细胞的各种代谢调节因子的转录，并增加调节葡萄糖和脂质代谢的基因的表达。罗格列酮用于治疗II型糖尿病患者，因为它通过对脂肪组织中脂肪酸的摄取和储存或对放射因子的影响，具有改善胰岛素敏感性的强大能力。
Reference
[1].Peter J. Cox, David A. Ryan, Frank J. Hollis, Ann-Marie Harris, Ann K. Miller, Marika Vousden and Hugh Cowley. Absorption, disposition, and metabolism of rosiglitazone, a potent thiazolidinedione insulin sensitizer, in humans. Drug Metabolism and Disposition 2000; 28(7): 772-780
[2].Adie Vilioen and Alan Sinclair. Safety and efficacy of rosiglitazone in the elderly diabetic patient. Vascular Health and Risk Management 2009:5 389-395
| Cas No. | 122320-73-4 | SDF | |
| 别名 | 罗格列酮; BRL 49653 | ||
| 化学名 | 5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3 | ||
| 分子式 | C18H19N3O3S | 分子量 | 357.43 |
| 溶解度 | ≥ 17.85 mg/mL in DMSO | 储存条件 | Store at 2-8°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 | 2.7978 mL | 13.9888 mL | 27.9775 mL |
| 5 mM | 0.5596 mL | 2.7978 mL | 5.5955 mL |
| 10 mM | 0.2798 mL | 1.3989 mL | 2.7978 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。