切换导航

Rosiglitazone

现货
Catalog No.
A4304
有效的PPARγ激动剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 500.00
现货
25mg
¥ 500.00
现货
100mg
¥ 700.00
现货
200mg
¥ 1,100.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

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.

Reference

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

Adie Vilioen and Alan Sinclair. Safety and efficacy of rosiglitazone in the elderly diabetic patient. Vascular Health and Risk Management 2009:5 389-395

Chemical Properties

StorageStore at -20°C
M.Wt357.43
Cas No.122320-73-4
FormulaC18H19N3O3S
SynonymsBrl-49653,Brl 49653
Solubility≥17.85 mg/mL in DMSO, <2.38 mg/mL in EtOH, <2.39 mg/mL in H2O
Chemical Name5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione
SDFDownload SDF
Canonical SMILESCN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

非小细胞肺癌(NSCLC)细胞(H1792和H1838)

溶解方法

该化合物在DMSO中的溶解度大于17.9 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

10 μmol/L,48小时

应用

Rosiglitazone降低了非小细胞肺癌(NSCLC)细胞(H1792和H1838)中Akt的磷酸化,增加磷酸酶和张力蛋白同源物(PTEN)蛋白表达,进而抑制NSCLC细胞增殖。Rosiglitazone增加了AMP活化蛋白激酶α(AMPKα)的磷酸化,AMPKα是LKB1的下游激酶靶标,Rosiglitazone降低p70核糖体蛋白S6激酶(p70S6K)的磷酸化,p70核糖体蛋白S6激酶是mTOR的下游靶标。

动物实验 [2]:

动物模型

C57/BL6小鼠

给药剂量

每天8 mg/kg

应用

在C57/BL6小鼠中进行股骨血管成形术,rosiglitazone (8 mg/kg/天)减轻新生内膜形成。在BM移植模型中,rosiglitazone将人内皮祖细胞的集落形成增加6倍,促进小鼠体内BM和人体外外周血中APC向内皮细胞系的分化,并抑制其向平滑肌细胞系的分化。在新内膜内,rosiglitazone刺激APCs分化为成熟的内皮细胞,并引起早期再内皮化。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

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.

质量控制

化学结构

Rosiglitazone