Troglitazone (Romglizone) is a PPARγ agonist with oral activity. Troglitazone has hypoglycemic activity, improves insulin resistance, and enhances insulin action. Troglitazone also has anti-inflammatory and anti-tumor activity.

PPARγ (human):550 nM (EC50), PPARγ (murine):780 nM (EC50)

方法：人胰腺癌细胞 MIA Paca2 和 PANC-1 用 Troglitazone (0-200  µM) 处理 24 h，使用 fluorescence assay 测定细胞活力。
结果：Troglitazone 对 MIA Paca2 和 PANC-1 细胞显示出剂量依赖性细胞毒性，IC50 值分别为 49.9 ± 1.2 µM 和 51.3 ± 5.3 µM。[1]
方法：人肺癌细胞 A549 用 Troglitazone (1-4  µM) 处理 12 h，使用 Western Blot 检测靶点蛋白表达水平。
结果：在不同浓度的 Troglitazone 下，DR4 和 DR5 的蛋白质表达水平没有变化。Troglitazone 治疗后，自噬标记物 LC3-II 显著增加，p62 以剂量依赖的方式降低。[2]

方法：为测试体内抗肿瘤活性，将 Troglitazone (200 mg/kg in 0.5% methylcellulose solution) 口服给药给携带人胰腺癌肿瘤 MIA-Paca2 的 Balb/c 小鼠，每天一次，持续五周。
结果：Troglitazone 在 MIA-Paca2 异种移植物模型中对肿瘤生长表现出抑制作用。[1]

Standard incubation mixtures (final volume of 0.20 mL) containe recombinant P450 (0.010 μM) in 50 mM potassium phosphate bu?er (pH 7.4) containing an NADPH-generating system (0.5 mm NADP+, 5 mM glucose 6-phosphate, 0.5 unit glucose 6-phosphate dehydrogenase/mL) and substrates (1±100 lM). For determination of CYP1A2, CYP2B6, CYP2E1 and CYP3A4 activities, 100 mM potassium phosphate buffer (pH 7.4) is used. When human liver microsomes are used as the enzyme source, 500, 25, 100 and 25 pmol totalP450 per mL are used for paclitaxel 6a-hydroxylation, S-warfarin 7-hydroxylation,S-mephenytoin 4′-hydroxylation and testosterone 6b-hydroxylation respectively.

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.