Home Metabolism PPAR agonist - TRP Channel modulator - Autophagy activator - Ferroptosis inhibitor Rosiglitazone maleate For research use only.

Rosiglitazone maleate

Synonyms: BRL-49653C, BRL-49653

Rosiglitazone maleate, 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 maleate Chemical Structure

Rosiglitazone maleate Chemical Structure

CAS No. 155141-29-0

Purity & Quality Control

Rosiglitazone maleate Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells Function assay Peroxisome proliferator activated receptor gamma agonistic activity in HepG2 cells, EC50=0.73 μM 10714503
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Biological Activity

Description Rosiglitazone maleate, 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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02737709 Terminated
Non-small Cell Lung Cancer
Sun Yat-sen University
 March 2016 Phase 2
NCT01402076 Completed
Healthy Volunteers
Vanda Pharmaceuticals
 August 2011 Phase 1
NCT01415128 Completed
Erectile Dysfunction
VIVUS LLC
 April 2010 Phase 1
NCT01100619 Completed
Papillary Thyroid Cancer|Follicular Thyroid Cancer|Huerthle Cell Thyroid Cancer|Renal Cell Carcinoma
Exelixis
 April 2010 Phase 1
NCT01376063 Completed
Healthy Adult Subjects
FibroGen
 March 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 473.5 Formula

C18H19N3O3S.C4H4O4
CAS No. 155141-29-0 SDF Download Rosiglitazone maleate SDF
Smiles CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (200.63 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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