Rosiglitazone maleate

Catalog No.S2505 Synonyms: BRL 49653

Rosiglitazone maleate Chemical Structure

Molecular Weight(MW): 473.5

Rosiglitazone, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ with IC50 of 42 nM.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
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Cited by 5 Publications

3 Customer Reviews

  • Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast.

    Mol Metab 2013 2(3), 215-26. Rosiglitazone maleate purchased from Selleck.

    Effect of rosiglitazone (RSG) treatment on neutrophil shift toward an N2 phenotype.Representative photomicrographs showing Ym1 (green) and neutrophils (red) double immunostaining 24 (upper) and 48 hours (lower) after permanent middle cerebral artery occlusion (pMCAO) in vehicle (VEH)- or RSG-treated mice.

    Stroke 2013 44(12), 3498-508. Rosiglitazone maleate purchased from Selleck.

  • Reprod Toxicol, 2016, 61:162-8. Rosiglitazone maleate purchased from Selleck.

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Biological Activity

Description Rosiglitazone, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ with IC50 of 42 nM.
Targets
PPARγ [1]
42 nM
In vitro

Rosiglitazone is an insulin-sensitising agent of the thiazolidinedione class of oral antihyperglycaemic drugs. Rosiglitazone exhibits insulin-sensitising activity 60- to 200-fold higher than that of troglitazone, englitazone, or piogliazone in rodent models of insulin ressitance. Rosiglitazone reduces hyperglycaemia by improving insulin sensitivity in adipose tissue, the liver and skeletal muscle tissue. Such insulin sensitisation may be partly attributable to the effects of Rosiglitazone on the expression of molecules involved in the insulin signalling cascade. In adipose tissue, Rosiglitazone-mediated PPARγ stimulation promotes adipocyte differentiation. Rosiglitazone may also promote the uptake of free fatty acids in adipose tissue, thus reducing systemic free fatty acid levels. The insulin sensitivity of the liver and peripheral tissues may be modulated indirectly by Rosiglitazone-mediated changes in levels of fatty acid or adipocyte-derived factors, such as adiponectin and TNFα. Rosiglitazone may also be involved in modulating the expression of adiponectin receptors in some tissues, which may be relevant to some aspects of insulin sensitisation. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells MmrhSpVv[3Srb36gZZN{[Xl? MXPQ[ZJwgGm|b33lJJBzd2yrZnXyZZRweiCjY4TpeoF1\WRicnXj[ZB1d3JiZ3HtcYEh[WexbnnzeIlkKGGldHn2bZR6KGmwIFjldGczKGOnbHzzMEBGSzVyPUCuO|Mh|ryP NYf5fVV5OTB5MUS1NFM>

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Protocol

Solubility (25°C)

In vitro DMSO 94 mg/mL (198.52 mM)
Water Insoluble
Ethanol Insoluble

* 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 473.5
Formula

C18H19N3O3S.C4H4O4

CAS No. 155141-29-0
Storage powder
in solvent
Synonyms BRL 49653

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03309319 Recruiting Pituitary Tumor Zhaoyun Zhang|Huashan Hospital October 16 2016 Not Applicable
NCT03309319 Recruiting Pituitary Tumor Zhaoyun Zhang|Huashan Hospital October 16 2016 Not Applicable
NCT02694874 Recruiting Malaria Centro de Investigacao em Saude de Manhica|University Health Network Toronto|Barcelona Institute for Global Health February 2016 Not Applicable
NCT02694874 Recruiting Malaria Centro de Investigacao em Saude de Manhica|University Health Network Toronto|Barcelona Institute for Global Health February 2016 Not Applicable
NCT01402076 Completed Healthy Volunteers Vanda Pharmaceuticals August 2011 Phase 1
NCT01287598 Completed Neoplasms Bayer August 2 2011 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID