Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Troglitazone (Romglizone) 是一种 PPARγ 激动剂,具有抗炎和抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 266 | 现货 | ||
5 mg | ¥ 397 | 现货 | ||
10 mg | ¥ 651 | 现货 | ||
25 mg | ¥ 1,350 | 现货 | ||
50 mg | ¥ 2,230 | 现货 | ||
100 mg | ¥ 3,930 | 现货 | ||
500 mg | ¥ 8,650 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 716 | 现货 |
产品描述 | Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity. |
靶点活性 | PPARγ (human):550 nM (EC50), PPARγ (murine):780 nM (EC50) |
体外活性 | 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. |
体内活性 | 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. |
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. |
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. |
别名 | CS-045, Romozin, Rezulin, Romglizone, Noscal, Prelay, 曲格列酮 |
分子量 | 441.54 |
分子式 | C24H27NO5S |
CAS No. | 97322-87-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 4.4 mg/mL (10 mM)), Heating is recommended.
DMSO: 44.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.2648 mL | 11.324 mL | 22.648 mL | 56.62 mL |
5 mM | 0.453 mL | 2.2648 mL | 4.5296 mL | 11.324 mL | |
10 mM | 0.2265 mL | 1.1324 mL | 2.2648 mL | 5.662 mL | |
DMSO | 20 mM | 0.1132 mL | 0.5662 mL | 1.1324 mL | 2.831 mL |
50 mM | 0.0453 mL | 0.2265 mL | 0.453 mL | 1.1324 mL | |
100 mM | 0.0226 mL | 0.1132 mL | 0.2265 mL | 0.5662 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Troglitazone 97322-87-7 Apoptosis Autophagy DNA Damage/DNA Repair Metabolism Ferroptosis PPAR Peroxisome proliferator-activated receptors CS-045 Inhibitor Romozin Rezulin Romglizone Noscal CS 045 CS045 inhibit Prelay 曲格列酮 inhibitor