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