S81177 |
Troglitazone |
源叶(MedMol) | 96% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)