产品说明书
Troglitazone
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同义名 : | CS-045;Romglizone;Rezulin, Resulin, Romozin, Noscal.;Prelay;GR 92132X;CI-991 |
| CAS号 : | 97322-87-7 | |
| 货号 : | A137444 | |
| 分子式 : | C24H27NO5S | |
| 纯度 : | 98% | |
| 分子量 : | 441.54 | |
| MDL号 : | MFCD00878416 | |
| 存储条件： |
粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(271.78 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 4 mg/mL clear PO 0.5% CMC-Na 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Troglitazone is a selective thiazolidinedione-based PPARγ agonist with EC50 values of 780nM and 550nM for PPAR-GAL4 transactivation assay of murine receptor and human receptor, respectively, with no obvious effect on PPARα and PPARδ up to 10μM[1]. Troglitazone is used as an antidiabetic agent. It has hypoglycemic effects in insulin-resistant animal models and non-insulin-dependent diabetic humans. Also its effect on acute increase in vivo insulin action in normal rats has also been found[2]. Troglitazone led a time-(50μM, 1-7days) and dose (50-100μM, in 3 days)-dependent antiproliferative effect on HL-60 cells, with effect on cell arrest at the G1 phase and differentiation into monocytes by Troglitazone found[3]. Similar antiproliferation and redifferentiation effect on thyroid cancer cell lines has also been found. Troglitazone-induced downregulation of surface expression of CD97, a novel dedifferentiation marker, in FTC-133 cells, and upregulation of sodium iodide symporter (NIS) mRNA in both TPC-1 and FTC-133 cells could be observed[4]. Troglitazone dose‑dependently inhibited cell migration and invasion of PC‑3 cells within 6-24h at concentration of 1, 10 and 40μM and increased the mRNA and protein levels of E‑cadherin and glutathione peroxidase 3 (GPx3) at concentration of 10μM after 24h[5]. | ||
| 作用机制 | Troglitazone thiazolidinedione-based PPARγ agonist which may directly bind to the AF-2 helix and stabilize the formation of the charge clamp on the surface of PPAR critical for recruitment of coactivator proteins to the receptor complex through their LxxLL motifs.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 3T3L1 cells | Function assay | Increase in 2-deoxyglucose uptake in mouse 3T3L1 cells at 3 uM by liquid scintillation counter | 18477507 | ||
| 3T3L1 cells | Function assay | Agonist activity at PPARgamma in mouse 3T3L1 cells, EC50=1 μM | 21493073 | ||
| 3T3-L1 cells | Function assay | Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.13 μM | 9599241 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02456428 | - | Completed | - | Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 << | |
| NCT03492580 | - | Completed | - | United States, New Jersey ... 展开 >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 收起 << | |
| NCT02476760 | - | Completed | - | Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.32mL 2.26mL 1.13mL |
22.65mL 4.53mL 2.26mL |
| 参考文献 |
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