| 名称 | Troglitazone |
| 描述 | 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. |
| 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. |
| 激酶实验 | 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. |
| 体外活性 | 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] |
| 体内活性 | 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] |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 4.4 mg/mL (10 mM)), Heating is recommended.
DMSO : 18.33 mg/mL (41.51 mM), Sonication is recommended.
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| 关键字 | Troglitazone | PPARγ | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | Ferroptosis | CS045 | CS 045 | Autophagy | Apoptosis |
| 相关产品 | Naringin | Guanidine hydrochloride | Daidzein | Gefitinib | Cysteamine hydrochloride | Alginic acid | Dextran sulfate sodium salt (MW 5000) | Hydroxychloroquine | Stavudine | L-Ascorbic acid sodium salt | Paeonol | Sodium 4-phenylbutyrate |
| 相关库 | 抗癌上市药物库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 抗衰老化合物库 | FDA 上市药物库 | DNA 损伤和修复分子库 | 免疫/炎症分子化合物库 | 神经退行性疾病化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |