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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Cited by 17 Publications

5 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.

  • 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

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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.
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3-L1 cells NUPjV5FETnWwY4Tpc44h[XO|YYm= MnPZSYZn\WO2aY\lJINwdmOnboTyZZRqd25iZn;yJIVvcGGwY3Xt[Y51KG:oIHnud5VtcW5vaX7keYNm\CC2cnnncJlk\XKrZHWgZYNkfW23bHH0bY9vKGmwIEPUN{1NOSClZXzsd{whTUN|ME2wMlAzKM7:TR?= MUOxOFUxPTZ2NB?=
COS1 cells M1LL[mZ2dmO2aX;uJIF{e2G7 NHjRbFRC\2:waYP0bYMh[WO2aY\peJkhf2G|IHTleIVzdWmwZXSgbY4hS0:VMTDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKEeDTDC0MXBRSVJiZ3HtcYEhemWlZYD0c5ItKEWFNUC9NE4xOjFizszN MlK3NVI3OTd7MkS=
CV-1 MlS2SpVv[3Srb36gZZN{[Xl? NGDwd4VKdiC4aYTyc{B1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBw\iCSZYLvfIl{d22nIIDyc4xq\mW{YYTvdkBi[3SrdnH0[YQhemWlZYD0c5Ih\2GvbXGgLHBRSVJrIHX4dJJme3OnZDDpckBEXi1zIHPlcIx{NCCHQ{WwQVAvODZizszN M4e2Rlg2PzZ7MEe=
HepG2 MUHGeY5kfGmxbjDhd5NigQ>? NFnGdnNG\m[nY4TpeoUh[2:wY3XueJJifGmxbjDh[4FqdnO2IHj1cYFvKFCSQWLnZY1u[SCneIDy[ZN{\WRiaX6gTIVxTzJiY3XscJMtKEWFNUC9NE4xOiEQvF2= NFXRU2cyPThyMUixOy=>
Huh7 MXXGeY5kfGmxbjDhd5NigQ>? NHfrSHBHfW6ldHnvcoFtKGGldHn2bZR6KGG2IHj1cYFvKFCSQWKg[4FudWFiaX6gTJVpPyClZXzsd{BjgSC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTB;MD6yNkDPxE1? M4\oVlE3OzZ4NkCx
U2OS cells MWLGeY5kfGmxbjDhd5NigQ>? MVPF[oZm[3Rib36gVHBCWmejbX3hJJRz[W6|YXP0bZZifGmxbjDhZ5Rqfmm2eTDpckBWOk:VIHPlcIx{NCCHQ{WwQVAvODNizszN M3zY[FE3OzByOUS0
HT29 M1jBd3Bzd2yrZnXyZZRqd25iYYPzZZk> Mki5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVEK5JINmdGxibHnu[UwhUUN3ME20OUDPxE1? M3jSelE3QDJzN{[5
NIH3T3 NVLVeHpuTnWwY4Tpc44h[XO|YYm= MX3BZ5Rqfmm2eTDheEBpfW2jbjDQVGFTKGejbX3hJJRz[W6|ZnXjeIVlKGmwIF7JTFNVOyClZXzsd{BjgSCudXPp[oVz[XOnIHHjeIl3cXS7IHHzd4F6NCCHQ{WwQVAvOzJizszN M{Pne|E3QDV2MEi1
HEK293 NVuwRVhGTnWwY4Tpc44h[XO|YYm= NHHxcohC[3Srdnn0fUBifCCqdX3hckBi\Gmyb4PlJJRqe3O3ZTDQVGFTKGejbX3hJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZpkhWFCDUj3HRWw1KHS{YX7zZYN1cX[jdHnvckBie3OjeTygSWM2OD1yLkOxJO69VQ>? NX\Eb5lrOTd|NEOzO|E>
CV1 NVPPT2RVTnWwY4Tpc44h[XO|YYm= NHX4dG0zPCCq NWO1RYdpSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBRWEGUYXzwbIEhcW5iQ2[xJINmdGy|IHL5JGdCVDRidILhcpNi[3SrdnH0bY9vKGG|c3H5JIFnfGW{IEK0JIhzeyxiRVO1NF0{NjR4IN88US=> MXKxO|UxPzJ{NR?=
293H DA M3jVNWZ2dmO2aX;uJIF{e2G7 MUixOkBp NGHRWJRC\2:waYP0JIFkfGm4aYT5JIF1KFCSQWLnZY1u[SCOQlSgbY4hcHWvYX6gNlk{UCCGQTDj[YxteyCjZoTldkAyPiCqcoOgZpkhXFJvRmLFWEBi[3SrdnH0bY9vKHKncH;yeIVzKGG|c3H5MEBGSzVyPUCuNFAzPCEQvF2= M4nzTVIzPTh{OUez
MDA-MB-231 NUnwZllST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3v4VlI1KGh? NXPSU24yT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjCyOEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWuNlMh|ryP NGXHemIzPTJ5OEKzOi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin D1 / CDK2 / CDK4 / Bax / Bcl-2 ; 

PubMed: 29725405     


A431 cells at 80% confluence were stimulated with rosiglitazone for 24 h, and the effects on Bax, Bcl-2, cyclin D1, cdk2 and cdk4 expression were analyzed by western blotting. Data were quantified by scanning densitometry, and the ratio of the protein of interest was normalized to GAPDH. Data are presented as means ± SEM (n=3). #P<0.05 (10, 20, 30, 40 mM rosiglitazone treatment compared with control treatment for cyclin D1/GAPDH and Cdk4/GAPDH; 30, 40 mM rosiglitazone treatment compared with control treatment for Cdk2/GAPDH) as analyzed with one-way ANOVA. 

29725405
Immunofluorescence
PPARγ / E-cadherin ; 

PubMed: 27145370     


Increased PPARγ (green) and E-cadherin (red) with rosiglitazone treatment and overlaid image showing colocalization (yellow, arrows) in high glucose condition (30 mM).

27145370
Growth inhibition assay
Cell viability ; 

PubMed: 29725405     


MTS assay of A431 cell viability. A431 cells were incubated with different concentrations (0–100 µM) rosiglitazone for 24 h. Cell viability was determined by MTS assay kit. Data are presented as the mean ± standard deviation of three independent experiments. #P<0.05 (0 µM rosiglitazone vs. 100 µM rosiglitazone) as analyzed with one-way analysis of variance.

29725405
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

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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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PPAR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID