Catalog No.S2556 Synonyms: BRL 49653
Molecular Weight(MW): 357.43
Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action.
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Treating a-galactosylceramide (a-GalCer)-injected mice with rosiglitazone partially restored the T-cell numbers in the spleen but not in the decidua. Number of T cells (a,d), CD41 T cells (b,e) and CD81 T cells (c,f) in the spleen and decidua from mice injected with a-GalCer, rosiglitazone (Rosi) or a-GalCer plus rosiglitazone (n=6-8 each).
Clin Exp Immunol, 2017, 189(2):211-225. Rosiglitazone purchased from Selleck.
Purity & Quality Control
Choose Selective PPAR Inhibitors
|Description||Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action.|
Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. Rosiglitazone has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. Rosiglitazone activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase.  Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro. Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected.  Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes. 
|In vivo||Rosiglitazone administration results in significant bone loss, including a decrease in bone volume, trabecular width, and trabecular number and an increase in trabecular spacing. Rosiglitazone also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. Rosiglitazone decreases the expression of the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen, whereas the expression of the adipocyte-specific fatty acid binding protein aP2 is increased.  Rosiglitazone upregulates gene transcripts encoding mitochondrial proteins in white adipocytes from ob/ob mice accompanied by an increase in mitochondrial mass and changes in mitochondrial structure. |
|In vitro||DMSO||71 mg/mL (198.64 mM)|
|In vivo||Add solvents to the product individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00064727||Completed||Congestive Heart Failure||National Heart, Lung, and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)||July 9, 2003||Phase 2|
|NCT02694874||Recruiting||Malaria||Centro de Investigacao em Saude de Manhica|University Health Network, Toronto|Barcelona Institute for Global Health||February 2016||--|
|NCT01402076||Completed||Healthy Volunteers||Vanda Pharmaceuticals||August 2011||Phase 1|
|NCT01287598||Active, not recruiting||Neoplasms||Bayer||August 2011||Phase 1|
|NCT01209143||Completed||Solid Cancers||Genentech, Inc.||November 2010||Phase 1|
|NCT01100619||Completed||Papillary Thyroid Cancer|Follicular Thyroid Cancer|Huerthle Cell Thyroid Cancer|Renal Cell Carcinoma||Exelixis||April 2010||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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