化合物信息

DB00412 

S2556 

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]

R2408 

Biochem/physiol Actions
Rosiglitazone is a potent agonist for PPARγ with an EC50 of 43 nM for the human receptor. It is antidiabetic, working as an insulin sensitizer by binding to the PPARγ receptors in fat cells and making the cells more responsive to insulin.