Rosiglitazone (BRL-49653) maleate
For research use only.
CAS No. 155141-29-0
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.
Selleck's Rosiglitazone (BRL-49653) maleate has been cited by 19 publications
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|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.|
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. 
|In vitro||DMSO||94 mg/mL (198.52 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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 Inc.||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|
|NCT01045590||Completed||Drug: titration||Diabetes Mellitus Type 2||GlaxoSmithKline||December 2003||Phase 4|
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