Rosiglitazone
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
过氧化物酶体增殖物激活受体γ(PPARγ)是核受体超家族的亚家族,多在脂肪组织中表达,响应于配体结合,调控基因表达,Rosiglitazone是其有效的激动剂。Rosiglitazone属于噻唑烷二酮(TZD)类,与其他TZD成员相似,可与PPARγ DNA结合为异二聚体,激活多种与干细胞分化为脂肪细胞有关的代谢调节子的转录,并增加调节葡萄糖和脂肪代谢的基因的表达。Rosiglitazone通过对脂肪组织中脂肪酸摄取和储存或对脂肪因子的效应,具有强烈提高胰岛素敏感性的能力,可用于II型糖尿病的治疗。
参考文献:
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
- 1. WeijieSuna, XiaoyuDuana, et al. "Adipogenic activity of 2-ethylhexyl diphenyl phosphate via peroxisome proliferator-activated receptor γ pathway." Science of The Total Environment. Available online 18 November 2019, 134810.
- 2. LianyingZhangab, WeijieSuna, et al. "Promoting differentiation and lipid metabolism are the primary effects for DINP exposure on 3T3-L1 preadipocytes." Environmental Pollution. Available online 13 September 2019, 113154.
Storage | Store at -20°C |
M.Wt | 357.43 |
Cas No. | 122320-73-4 |
Formula | C18H19N3O3S |
Synonyms | Brl-49653,Brl 49653 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥17.85 mg/mL in DMSO |
Chemical Name | 5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione |
SDF | Download SDF |
Canonical SMILES | CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
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