Rosiglitazone (BRL-49653) maleate

Catalog No.S2505

For research use only.

Rosiglitazone maleate (BRL 49653), a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.

Rosiglitazone (BRL-49653) maleate Chemical Structure

CAS No. 155141-29-0

Selleck's Rosiglitazone (BRL-49653) maleate has been cited by 23 publications

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Biological Activity

Description Rosiglitazone maleate (BRL 49653), a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. Rosiglitazone maleate also modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis.
Targets
Ferroptosis [2] 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 MkPESpVv[3Srb36gZZN{[Xl? NXX4[lhXWGW{b4jpd49u\SCycn;sbYZmemG2b4KgZYN1cX[jdHXkJJJm[2WydH;yJIdidW2jIHHnc45qe3SrYzDhZ5Rqfmm2eTDpckBJ\XCJMjDj[YxteyxiRVO1NF0xNjd|IN88US=> MkDRNVA4OTR3MEO=

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 473.5
Formula

C18H19N3O3S.C4H4O4

CAS No. 155141-29-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3.C(=CC(=O)O)C(=O)O

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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
NCT01415128 Completed Drug: Omeprazole|Drug: Rosiglitazone|Drug: Desipramine Erectile Dysfunction VIVUS LLC April 2010 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
NCT01376063 Completed Drug: FG-4592 Healthy Adult Subjects FibroGen March 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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