Rosiglitazone

Catalog No.S2556 Synonyms: BRL 49653

Rosiglitazone  Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
USD 220 In stock
USD 370 In stock
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3 Customer Reviews

  • J Leukoc Biol 2014 95(4), 587-98. Rosiglitazone purchased from Selleck.

    J Leukoc Biol 2014 95(4), 587-98. Rosiglitazone purchased from Selleck.

  • 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

Biological Activity

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.
Targets
PPAR [1]
(Cell-free assay)
In vitro

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. [1] Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.[2] Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. [3] Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes. [4]

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. [2] 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. [4]

Protocol

Solubility (25°C)

In vitro DMSO 71 mg/mL (198.64 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 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.

Chemical Information

Molecular Weight 357.43
Formula

C18H19N3O3S

CAS No. 122320-73-4
Storage powder
Synonyms BRL 49653

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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

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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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PPAR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID