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Rosiglitazone

Catalog No.
A4304
Potent PPARγ agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
25mg
$50.00
In stock
100mg
$70.00
In stock
200mg
$110.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

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Email: [email protected]

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Background

Rosiglitazone (CAS: 122320-73-4) is a synthetic thiazolidinedione (TZD) that functions as an agonist of peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear receptor highly expressed in adipose tissues. Upon ligand binding, PPARγ forms heterodimers with retinoid X receptors, promoting transcriptional activation of genes regulating adipogenesis, glucose uptake, lipid metabolism, and insulin sensitivity. Through modulating fatty acid storage in adipose tissue and secretion of adipokines, rosiglitazone significantly enhances insulin sensitivity, making it extensively utilized in metabolic and diabetes research, particularly type II diabetes studies.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt357.43
Cas No.122320-73-4
FormulaC18H19N3O3S
SynonymsBrl-49653, Brl 49653
Solubilityinsoluble in EtOH; insoluble in H2O; ≥17.85 mg/mL in DMSO
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
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

Non-small cell lung carcinoma (NSCLC) cells (H1792 and H1838)

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°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Reacting condition

10 μmol/L, 48 hours

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]:

Animal models

C57/BL6 mice

Dosage form

8 mg/kg per day

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.

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.

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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