Troglitazone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种 PPARγ 激活剂，具有抗糖尿病、抗肿瘤和抗炎活性。

A PPARγ activator that has antidiabetic, anti-tumor and anti-inflammatory activities; binds to PPARγ and selectively induces the early growth response-1 gene expression; inhibits biosynthesis of cholesterol in CHO cell (IC50=8 ug/ml); enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux.Diabetes Approved(In Vitro):Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine?PPARγ receptor, respectively. Troglitazone (2-200 μM) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 and PANC-1 cells), with IC50s of 49.9?±?1.2 and 51.3?±?5.3 μM, respectively. Troglitazone (50 μM) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression. Troglitazone (0, 1, 2, and 4 μM) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells. Troglitazone enhancement of TRAIL-induced apoptosis is blocked by inhibition of autophagy, via activation of autophagy flux. In addition, the effects of troglitazone are induced by PPARγ activation in A549 cells.(In Vivo):Troglitazone (200 mg/kg, p.o.) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model.

Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine?PPARγ receptor, respectively. Troglitazone (2-200 μM) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 and PANC-1 cells), with IC50s of 49.9?±?1.2 and 51.3?±?5.3 μM, respectively. Troglitazone (50 μM) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression. Troglitazone (0, 1, 2, and 4 μM) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells. Troglitazone enhancement of TRAIL-induced apoptosis is blocked by inhibition of autophagy. In addition, the effects of troglitazone are induced by PPARγ activation in A549 cells.

Troglitazone (200 mg/kg, p.o.) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model.

CS-045

Metabolic Enzyme/Protease

PPAR

PPARγ

Metabolic Disease

Diabetes

97322-87-7

441.5399

C24H27NO5S

>98% (HPLC)

10 mM in DMSO

O=C(N1)SC(CC2=CC=C(OCC3(C)CCC4=C(C)C(O)=C(C)C(C)=C4O3)C=C2)C1=O

2,4-Thiazolidinedione, 5-[[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years