| 产品描述: | Troglitazone is a PPARγ agonist with anti-inflammatory and anti-tumor activity. |
| 靶点: |
Apoptosis;Autophagy;Ferroptosis;PPAR;Apoptosis; Ferroptosis; PPAR; Autophagy |
| 体外研究: |
Troglitazone inhibits the growth of 786-O and A498 cells with EC50 values of 5.71 μM and 8.38 μM. Troglitazone(5 μM) significantly inhibits the CYP2C8-dependent paclitaxel 6a-hydroxylation and CYP2C9-dependent S-warfarin 7-hydroxylation. Troglitazone extensively suppresses CYP2C19-dependent S-mephenytoin 4´-hydroxylation and CYP3A4-dependent testosterone 6b-hydroxylation and moderately influences the CYP1A2- and CYP2B6-dependent 7-ethoxycoumarin O-deethylation, CYP2A6-dependent coumarin 7-hydroxylation and CYP2D6-dependent bufuralol 1´-hydroxylation. CYP2E1-dependent 7-ethoxycoumarin O-deethylation is not inhibited. |
| 体内研究: |
Local hypoxia is observed in liver but not in adipose tissue in troglitazone-treated mice. A significant increase in Ki-67/CD31 LI in liver, BAT, and WAT is observed in the 400 mg/kg troglitazone group. Troglitazone reduces the incidence of diabetes by 16 weeks compared to controls, when administered by gavage from weaning at a dose of 400 mg/kg body weight |
| 细胞实验: |
Troglitazone is made at 100 mM concentration in DMSO and added to the culture medium at the final concentration of less than 0.1%. The effect of PPARγ ligands on cell proliferation of RCC cells is determined using MTT assay. Briefly, cells of 0.5×l04 cells/well are inoculated into a 96-well plate, treated with pioglitazone or troglitazone at various concentrations. After an incubation for 24 h, 20 μL/well 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT, 5 g/L) is added to each well, the medium is then removed, and 200 μL of 0.04mol/LHCl in isopropanol is added to dissolve the reduced formazan product. The plate is read in a microplate reader at 590 nm. |
| 参考文献: |
1. Jaeschke H. Troglitazone hepatotoxicity: are we getting closer to understanding idiosyncratic liver injury?. Toxicol Sci. 2007, 97(1):1-3. 2. Baek SJ, et al. Troglitazone, a peroxisome proliferator-activated receptor gamma (PPAR gamma ) ligand, selectively induces the early growth response-1 gene independently of PPAR gamma. A novel mechanism for its anti-tumorigenic activity. J Biol Chem. 2003, 278(8):5845-53. 3. van Westerloo DJ, et al. Troglitazone, the peroxisome proliferator-activated receptor-gamma agonist, induces antiproliferation and redifferentiation in human thyroid cancer cell lines. Therapeutic effects of troglitazone in experimental chronic pancreatitis in mice. Am J Pathol. 2005, 166(3):721-8. 4. Park JW, et al. Troglitazone, the peroxisome proliferator-activated receptor-gamma agonist, induces antiproliferation and redifferentiation in human thyroid cancer cell lines. Thyroid. 2005, 15(3):222-31. 5. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91. 6. Bolden A, et al. The PPAR Gamma Agonist Troglitazone Regulates Erk 1/2 Phosphorylation via a PPARγ-Independent, MEK-Dependent Pathway in Human Prostate Cancer Cells. PPAR Res. 2012, 2012:929052. 7. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831. |
| 溶解性: |
Soluble in DMSO、Ethanol |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.265 ml |
11.324 ml |
22.648 ml |
| 5 mM |
0.453 ml |
2.265 ml |
4.53 ml |
| 10 mM |
0.226 ml |
1.132 ml |
2.265 ml |
| 50 mM |
0.045 ml |
0.226 ml |
0.453 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |