Rosiglitazone (Synonyms: BRL 49653)

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