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曲格列酮 /Troglitazone {[allProObj[0].p_purity_real_show]}

货号:A137444 同义名: CS-045;Romglizone

Troglitazone是一种口服活性的PPARγ激动剂,对人和小鼠PPARγ受体的EC50分别为550 nM和780 nM。它具有抗癌活性,并能预防和抑制2型糖尿病的发展。

Troglitazone 化学结构 CAS号:97322-87-7
Troglitazone 化学结构
CAS号:97322-87-7
Troglitazone 3D分子结构
CAS号:97322-87-7
Troglitazone 化学结构 CAS号:97322-87-7
Troglitazone 3D分子结构 CAS号:97322-87-7
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Troglitazone 纯度/质量文件 产品仅供科研

货号:A137444 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PPARα PPARβ/δ PPARγ PPARδ 其他靶点 纯度
Fenofibric acid 98%
GW6471 ++

PPARα, IC50: 0.24 μM

99%+
GSK3787 ++

PPARδ, pIC50: 6.6

++

PPARδ, pIC50: 6.6

99%+
FH535 98%+
GW9662 +++

PPARα, IC50: 32 nM

+++

PPARγ, IC50: 3.3 nM

98%
T0070907 ++++

PPARγ, IC50: 1 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Troglitazone 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]

Troglitazone 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
A549 Growth inhibition assay Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay, GI50=15 μM 15454234

Troglitazone 动物研究

Dose Rat: 0.05 mg/kg - 0.1 mg/kg[6] (p.o., BID); 25 mg/kg - 200 mg/kg[7] (female rats, p.o.) Mice: 10 mg/kg - 30 mg/kg[8] (i.p.); 50 mg/kg - 800 mg/kg[7] (p.o.) Pig: 10 mg/kg[9] (i.v.) Cynomolgus monkeys: 300 mg/kg - 1200 mg/kg[10] (p.o.)
Administration p.o., i.p., i.v.

Troglitazone 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 <<

Troglitazone 参考文献

[1]Willson TM, Brown PJ, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.

[2]Lee MK, Olefsky JM, et al. Acute effects of troglitazone on in vivo insulin action in normal rats. Metabolism. 1995 Sep;44(9):1166-9.

[3]Fujimura S, Suzumiya J, et al. Effects of troglitazone on the growth and differentiation of hematopoietic cell lines. Int J Oncol. 1998 Dec;13(6):1263-7.

[4]Park JW, Zarnegar R, et al. Troglitazone, the peroxisome proliferator-activated receptor-gamma agonist, induces antiproliferation and redifferentiation in human thyroid cancer cell lines. Thyroid. 2005 Mar;15(3):222-31.

[5]Chang SN, Lee JM, et al. Troglitazone inhibits the migration and invasion of PC-3 human prostate cancer cells by upregulating E-cadherin and glutathione peroxidase 3. Oncol Lett. 2018 Oct;16(4):5482-5488.

Troglitazone 实验方案

计算器
存储液制备 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

Troglitazone 技术信息

CAS号97322-87-7
分子式C24H27NO5S
分子量 441.54
别名 CS-045;Romglizone;Rezulin, Resulin, Romozin, Noscal.;Prelay;GR 92132X;CI-991
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

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

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

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