Troglitazone | CS-045 | PPARγ Agonist | AmBeed-信号通路专用抑制剂

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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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

PPAR 亚型比较

产品名称	PPARα ↓ ↑	PPARβ/δ ↓ ↑	PPARγ ↓ ↑	PPARδ ↓ ↑	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

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere,Store in freezer, under -20°C

溶解方案

细胞实验：

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

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
CHO cells		Function assay	24 h	Agonist activity at human PPARgamma expressed in CHO cells co-transfected with pGL3-PPRE3-TK-luc assessed as transactivation after 24 hrs by firefly luciferase reporter gene assay, EC50=0.44 μM	22342624
CHO cells		Function assay		Agonist activity at human recombinant PPARgamma expressed in CHO cells cotransfected with pGL3-PPRE3-TK-luc reporter assessed as beta-galactosidase activity at after 24 hrs by luciferase based transactivation assay, EC50=0.44 μM	22424300
CV1 cells		Function assay		Transactivation of human PPARgamma expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.4 μM	22579420
CV-1 cells		Function assay		Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.53703 μM	9836620
HEK293 cells		Function assay		Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
HEK293 cells		Function assay		Activation of PPARgamma transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control, EC50=0.4 μM	21800856
HEK293 cells	10 μM	Function assay	24 h	Transactivation of PPAR-gamma transfected in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	22579484
HEK293T cells		Function assay		Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5 Μm	23122865
HepG2 (DPX-2) cells		Function assay	24 h	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=6.9 μM	20966043
HepG2 cells		Function assay	20 h	Transactivation of GAL4-fused PPARgamma LBD expressed in HepG2 cells after 20 hrs by luminescence assay, EC50=0.73 μM	22381047
HepG2 cells	50 μM	Function assay	24 h	Induction of p53 protein level in human HepG2 cells at 50 uM up to 24 hrs by immunoblot analysis	25851939
HepG2 cells	0.5-12.5 μM	Function assay		Agonist activity at PPARgamma in human HepG2 cells assessed as down-regulation of glucose-6-phosphatase at 0.5 to 12.5 uM by real-time PCR method	22342624
HepG2 cells	0.5-12.5 μM	Function assay		Agonist activity at PPARgamma in human HepG2 cells assessed as down-regulation of phosphoenolpyruvate carboxykinase at 0.5 to 12.5 uM by real-time PCR method	22342624
HepG2 cells		Function assay		Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of phosphoenolpyruvate carboxykinase mRNA by RT-PCR analysis	22424300
HepG2 cells		Function assay		Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of glucose-6-phosphatase mRNA by RT-PCR analysis	22424300
HepG2 cells		Function assay		Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50=0.72 μM	23031596
LNCAP cells		Cytotoxicity assay	24 h	Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay, IC50=22 μM	22546208
MA104 cells		Cytotoxicity assay	24 h	Cytotoxicity against monkey MA104 cells after 24 hrs, TD50=18.5 μM	22365411
MCF7 cells		Proliferation assay	24 h	Antiproliferative activity hormone-dependent human MCF7 cells after 24 hrs by luminescent cell viability assay, IC50=35.4 μM	22409968
MDA-MB-231 cells		Proliferation assay	24 h	Antiproliferative activity hormone-independent human MDA-MB-231 cells after 24 hrs by luminescent cell viability assay, IC50=15.7 μM	22409968
PC12 cells		Proliferation assay		Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay, IC50=15 Μm	15109648
PC3 cells		Cytotoxicity assay	24 h	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50=30 μM	22546208
rat ventricular myocytes		Function assay		Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes, IC50=9.5 μM	22761000
ST-13 cells	5 μM	Function assay	11 days	Induction of preadipocyte differentiation in mouse ST-13 cells assessed as lipid accumulation at 5 uM within 11 days by oil red-staining relative to control	19268587

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 <<
NCT02475499	-		Completed	-	Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT01068860	Type 2 Diabetes Mellitus ... 展开 >> Impaired Glucose Tolerance 收起 <<	Phase 2	Completed	-	-
NCT00758719	-		Completed	-	United States, Indiana ... 展开 >> Union Hospital Neurosurgical Terre Haute, Indiana, United States, 47807 United States, Michigan Family Orthopedic Associates Flint, Michigan, United States, 48507 United States, Ohio Orthopedics and Neurological Consultants, Inc Columbus, Ohio, United States, 43212 United States, Wisconsin Neurological Associates of Waukesha Waukesha, Wisconsin, United States, 53188 收起 <<
NCT01068860	-		Completed	-	-
NCT01045590	Diabetes Mellitus, Type 2	Phase 4	Completed	-	Korea, Republic of ... 展开 >> GSK Investigational Site Seoul, Korea, Republic of, 110-744 GSK Investigational Site Seoul, Korea, Republic of, 120-752 GSK Investigational Site Seoul, Korea, Republic of, 135-710 GSK Investigational Site Seoul, Korea, Republic of, 137-701 收起 <<
NCT01055223	-		Completed	-	-
NCT00116545	Atherosclerosis ... 展开 >> Diabetes Mellitus 收起 <<	Phase 2 Phase 3	Completed	-	United States, California ... 展开 >> Atherosclerosis Research Unit, Division of Cardiovascular Medicine, Department of Medicine Los Angeles, California, United States, 90033 收起 <<
NCT00975169	-		Unknown	-	Taiwan ... 展开 >> Department of Internal Medicine, National Taiwan University Hospital Recruiting Taipei, Taiwan Contact: Linda Huang 886 9 67670020 linda590203@gmail.com Principal Investigator: Tien-Jyun Chang, Ph D 收起 <<
NCT01055223	-		Completed	-	-
NCT00003058	Sarcoma	Phase 2	Completed	-	United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 收起 <<

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

Troglitazone 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Troglitazone 质控信息

Troglitazone 生物活性

Troglitazone 细胞研究

Troglitazone 动物研究

Troglitazone 临床研究

Troglitazone 参考文献

Troglitazone 实验方案

Troglitazone 技术信息

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

Troglitazone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Troglitazone 质控信息

Troglitazone 生物活性

Troglitazone 细胞研究

Troglitazone 动物研究

Troglitazone 临床研究

Troglitazone 参考文献

Troglitazone 实验方案

Troglitazone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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