Rosiglitazone
Rosiglitazone is a thiazolidinedione insulin sensitizer that activates PPARγ, decreasing blood glucose and insulin levels. Rosiglitazone exhibits anti-diabetic, anti-inflammatory, antioxidative, anticancer, anti-angiogenic, antihypertensive, and anti-fibrotic activities. In vivo, rosiglitazone decreases LPS-stimulated production of TNF-α, IL-1β, and IL-6 as well as activity of myeloperoxidase; it also inhibits activation of NF-κB, preventing mastitis. In multiple myeloma cells, rosiglitazone suppresses expression of HIF-1α and IGF-1, decreases activation of Aky, and ERK, and inhibits cell viability and proliferation. This compound also inhibits endothelin-1-induced vasoconstriction in a NO-dependent manner in animal models of pulmonary arterial hypertension. Additionally, rosiglitazone prevents activation of AP-1, production of collagen, and differentiation in fibroblasts.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1896510
| Cas No. |
122320-73-4 |
|---|---|
| Purity |
≥98% |
| Formula |
C18H19N3O3S |
| Formula Wt. |
357.43 |
| Chemical Name |
5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]phenyl]- methyl]-2,4-thiazolidinedione |
| IUPAC Name |
5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione |
| Synonym |
BRL-49653 |
| Melting Point |
153-155°C |
| Solubility |
Soluble in ethanol and in buffered aqueous solutions (pH of 2.3). |
| Appearance |
White Crystal Powder |
Rui M, Huang Z, Liu Y, et al. Rosiglitazone suppresses angiogenesis in multiple myeloma via downregulation of hypoxia inducible factor 1α and insulin like growth factor 1 mRNA expression. Mol Med Rep. 2014 Jul 22. [Epub ahead of print]. PMID: 25050627.
Mingfeng D, Xiaodong M, Yue L, et al. Effects of PPAR-γ Agonist Treatment on LPS-Induced Mastitis in Rats. Inflammation. 2014 May 18. [Epub ahead of print]. PMID: 24839089.
Liu Y, Tian XY, Huang Y, et al. Rosiglitazone Attenuated Endothelin-1-Induced Vasoconstriction of Pulmonary Arteries in the Rat Model of Pulmonary Arterial Hypertension via Differential Regulation of ET-1 Receptors. PPAR Res. 2014;2014:374075. PMID: 24701204.
He H, Tao H, Xiong H, et al. Rosiglitazone causes cardiotoxicity via peroxisome proliferator-activated receptor γ-independent mitochondrial oxidative stress in mouse hearts. Toxicol Sci. 2014 Apr;138(2):468-81. PMID: 24449420.
Hou X, Zhang Y, Shen YH, et al. PPAR-γ activation by rosiglitazone suppresses angiotensin II-mediated proliferation and phenotypictransition in cardiac fibroblasts via inhibition of activation of activator protein 1. Eur J Pharmacol. 2013 Sep 5;715(1-3):196-203. PMID: 23791613.
