Rosiglitazone
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.
5 Customer Reviews
-
BV2 cells were pretreated with JuA for 30 min, followed by administration of Aβ42 (5 μM) for 12 h. Cells were fixed and immunostained with PPARγ antibody. The representative images demonstrate the amount and localization of PPARγ (green). Nuclei were counterstained with DAPI (blue). Scale bar: 40 μm.
Theranostics, 2018, 8(15):4262-4278. Rosiglitazone purchased from Selleck.
-
Rosiglitazone normalizes colon carcinoma vasculature and reduces tumor‐associated macrophage (TAM) infiltration. When CT26 tumor size approximately reached 50 mm3, the mice were given 100 mg/kg rosiglitazone or vehicle by oral gavage per day for 2 weeks. Then, the tumor samples were collected. A, Microvascular density and pericyte coverage were investigated by double immunofluorescence staining for CD31 and NG2. Scale bar, 50 μm. B, Multiphoton laser‐scanning microscopy images of CT26 tumor vasculature (green) stained with FITC‐dextran. Scale bar, 100 mm. C, Tumor vessel perfusion indicated by CD31‐positive endothelial cells stained red; FITC‐lectin perfused vessels are stained green. Scale bar, 50 μm. D, Representative micrographs show pimonidazole (PIMO)‐stained (green) CT26 tumor sections for hypoxia study. Scale bar, 100 μm. Hypoxic tumor regions are highlighted by dashed lines. E, Immunofluorescence staining for F4/80 showing TAM infiltration. Scale bar, 50 μm. Immunofluorescence images from (A to E) were captured within randomly selected fields (4‐6 fields per tumor, n = 6 mice). Data are presented mean ± SEM. **P < .01; ***P < .001
Cancer Sci, 2018, 109(7):2243-2255. 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 |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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] |
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Cell Data |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Assay |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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(Data is from Selleck tests instead of citations): 4% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. |
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 |
in solvent | |
Synonyms | BRL 49653 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
---|---|---|---|---|---|---|
NCT02737709 | Terminated | Drug: Paclitaxel and Carboplatin regimen | Non-small Cell Lung Cancer | Sun Yat-sen University | March 2016 | Phase 2 |
NCT01402076 | Completed | Drug: Tasimelteon|Drug: Rosiglitazone|Drug: Midazolam | Healthy Volunteers | Vanda Pharmaceuticals | August 2011 | Phase 1 |
NCT01100619 | Completed | Drug: rosiglitazone|Drug: XL184 | Papillary Thyroid Cancer|Follicular Thyroid Cancer|Huerthle Cell Thyroid Cancer|Renal Cell Carcinoma | Exelixis | April 2010 | Phase 1 |
NCT01415128 | Completed | Drug: Omeprazole|Drug: Rosiglitazone|Drug: Desipramine | Erectile Dysfunction | VIVUS Inc. | April 2010 | Phase 1 |
NCT01376063 | Completed | Drug: FG-4592 | Healthy Adult Subjects | FibroGen | March 2010 | Phase 1 |
Tech Support
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.