Research Area: Immunology
Biological Activity:
Rosiglitazone (Avandia) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone (Avandia) has recently been identified as a high-affinity ligand for PPARγ, a nuclear hormone receptor that is abundantly expressed in adipocytes and plays a central role as a regulator of terminal adipocyte differentiation. Rosiglitazone (Avandia) acts primarily by increasing insulin sensitivity. Rosiglitazone (Avandia) improves glycemic control while reducing circulating insulin levels. Rosiglitazone (Avandia) is a member of the thiazolidinedione class of drugs. They reduce glucose, fatty acid, and insulin blood concentrations. They work by binding to the peroxisome proliferator-activated receptors (PPARs). Thiazolidinediones enter the cell, bind to the nuclear receptors, and affect the expression of DNA. Rosiglitazone (Avandia, BRL-49653) also appears to have an anti-inflammatory effect in addition to its effect on insulin resistance. [1][2]