product name Rosiglitazone maleate
Description: Rosiglitazone maleate, the maleic acid salt form of rosiglitazone, is a member of the thiazolidinedione class of antihyperglycaemic agents. It is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ. Rosiglitazone maleate is a potent insulin sensitizer, which is used for the treatment of diabetes. Rosiglitazone improves the sensitivity of end organs to insulin through PPARγ activation which poteniates them to lower concentrations of blood glucose.
References: Drugs. 2007;67(18):2747-79.
473.5
Formula
C18H19N3O3S.C4H4O4
CAS No.
155141-29-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 94 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
BRL 49653
other peoduct :
| In Vitro |
In vitro activity: 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 sensitization. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Drugs. 2007;67(18):2747-79. |
