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Troglitazone

Troglitazone

产品编号 T3170   CAS 97322-87-7
别名: CS-045, Romozin, Rezulin, Romglizone, Noscal, Prelay, 曲格列酮

Troglitazone (Romglizone) 是一种 PPARγ 激动剂,具有抗炎和抗肿瘤活性。

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Troglitazone Chemical Structure
Troglitazone, CAS 97322-87-7
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Troglitazone (T3170)
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纯度: 99.62%
纯度: 99.36%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 4.4 mg/mL (10 mM)), Heating is recommended.

DMSO: 44.2 mg/mL (100 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Park JW, et al. Thyroid. 2005, 15(3):222-31. 2. Bolden A, et al. PPAR Res. 2012, 2012:929052. 3. Baek SJ, et al. J Biol Chem. 2003, 278(8):5845-53. 4. van Westerloo DJ, et al. Am J Pathol. 2005, 166(3):721-8. 5. Jaeschke H. Toxicol Sci. 2007, 97(1):1-3. 6. 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. 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.

TargetMol Library Books文献引用

1. Kazberuk A, Chalecka M, Palka J, et al. Nonsteroidal Anti-Inflammatory Drugs as PPARγ Agonists Can Induce PRODH/POX-Dependent Apoptosis in Breast Cancer Cells: New Alternative Pathway in NSAID-Induced Apoptosis. International Journal of Molecular Sciences. 2022, 23(3): 1510. 2. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989. 3. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200.
MPTP hydrochloride Nevanimibe hydrochloride Triciribine phosphate Torin 2 AEG 3482 OsMundacetone AZ960 Nimustine Hydrochloride

相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 抗癌活性化合物库 抗癌药物库 抗癌临床化合物库 药物功能重定位化合物库 抗癌上市药物库 抗纤维化化合物库 人代谢物化合物库 代谢化合物库 活性脂质化合物库

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Keywords

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

 

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