Rosiglitazone maleate 155141-29-0

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Molecular Weight:

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.






Biological 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 sensitisation.

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