货号：T2155

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

Troglitazone is a selective thiazolidinedione-based PPARγ agonist with EC50 values of 780nM and 550nM for PPAR-GAL4 transactivation assay of murine receptor and human receptor, respectively, with no obvious effect on PPARα and PPARδ up to 10μM. Troglitazone is used as an antidiabetic agent. It has hypoglycemic effects in insulin-resistant animal models and non-insulin-dependent diabetic humans. Also its effect on acute increase in vivo insulin action in normal rats has also been found. Troglitazone led a time-(50μM, 1-7days) and dose (50-100μM, in 3 days)-dependent antiproliferative effect on HL-60 cells, with effect on cell arrest at the G1 phase and differentiation into monocytes by Troglitazone found. Similar antiproliferation and redifferentiation effect on thyroid cancer cell lines has also been found. Troglitazone-induced downregulation of surface expression of CD97, a novel dedifferentiation marker, in FTC-133 cells, and upregulation of sodium iodide symporter (NIS) mRNA in both TPC-1 and FTC-133 cells could be observed. Troglitazone dosedependently inhibited cell migration and invasion of PC3 cells within 6-24h at concentration of 1, 10 and 40μM and increased the mRNA and protein levels of Ecadherin and glutathione peroxidase 3 (GPx3) at concentration of 10μM after 24h.

作用机制

Troglitazone thiazolidinedione-based PPARγ agonist which may directly bind to the AF-2 helix and stabilize the formation of the charge clamp on the surface of PPAR critical for recruitment of coactivator proteins to the receptor complex through their LxxLL motifs.

产品信息