The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs), a group of structurally related synthetic agonists with antidiabetic actions in vivo.{7575,8930} Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class.{8461} MCC-555 is a structural homolog of rosiglitazone and the other TZDs. MCC-555 binds with about 1/10 the affinity of rosiglitazone to PPARγ.{7413} Despite this, MCC-555 is a more potent antidiabetic agent in whole animal experiments than rosiglitazone and several other prototypic TZDs; the ED50 value in these experiments was 2.7 mg/kg for MCC-555 compared with 7.1 mg/kg for rosiglitazone. MCC-555 is therefore a unique new member of the TZD class and may be useful in differentiating some of the multiple activities attributed to this class of compounds.
产品描述
A structural homolog of rosiglitazone that binds PPARγ with about 1/10 the affinity of rosiglitazone yet is a more potent antidiabetic agent in whole animal experiments than rosiglitazone (ED50s = 2.7 mg/kg and 7.1 mg/kg, respectively)
