| 名稱 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 方法：人胰腺癌細(xì)胞 MIA Paca2 和 PANC-1 用 Troglitazone (0-200 ?μM) 處理 24 h，使用 fluorescence assay 測定細(xì)胞活力。
結(jié)果：Troglitazone 對 MIA Paca2 和 PANC-1 細(xì)胞顯示出劑量依賴性細(xì)胞毒性，IC50 值分別為 49.9?±?1.2 μM 和 51.3?±?5.3 μM。[1]
方法：人肺癌細(xì)胞 A549 用 Troglitazone (1-4 ?μM) 處理 12 h，使用 Western Blot 檢測靶點(diǎn)蛋白表達(dá)水平。
結(jié)果：在不同濃度的 Troglitazone 下，DR4 和 DR5 的蛋白質(zhì)表達(dá)水平?jīng)]有變化。Troglitazone 治療后，自噬標(biāo)記物 LC3-II 顯著增加，p62 以劑量依賴的方式降低。[2] |
| 體內(nèi)活性 | 方法：為測試體內(nèi)抗腫瘤活性，將 Troglitazone (200 mg/kg in 0.5% methylcellulose solution) 口服給藥給攜帶人胰腺癌腫瘤 MIA-Paca2 的 Balb/c 小鼠，每天一次，持續(xù)五周。
結(jié)果：Troglitazone 在 MIA-Paca2 異種移植物模型中對腫瘤生長表現(xiàn)出抑制作用。[1] |
| 存儲條件 | Store at low temperature
Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.53 mM), Sonication is recommended.
Ethanol : 4.4 mg/mL (9.97 mM), Heating is recommended.
DMSO : 18.33 mg/mL (41.51 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Troglitazone | PPARγ | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | Ferroptosis | CS045 | CS 045 | Autophagy | Apoptosis |
| 相關(guān)產(chǎn)品 | Formamide | Urea | Guanidine hydrochloride | Naringin | Daidzein | Aceglutamide | Alginic acid | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Paeonol |
| 相關(guān)庫 | 抗癌上市藥物庫 | 抗癌活性化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 免疫/炎癥分子化合物庫 | 神經(jīng)退行性疾病化合物庫 | 藥物功能重定位化合物庫 | 鐵死亡化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |