Home Metabolism PPAR agonist - Autophagy activator - Apoptosis related activator - Ferroptosis inhibitor Troglitazone 仅限科研使用

Troglitazone

别名: CS-045, Romglizone 中文名称：曲格列酮

Troglitazone是PPAR的有效激动剂，PPAR是配体激活的转录因，可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。

Troglitazone Chemical Structure

Troglitazone Chemical Structure

CAS: 97322-87-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1040.13 现货
10mg 958.57 现货
50mg 3661.39 现货
200mg 9582.31 现货
1g 32679 现货
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Troglitazone相关产品

相关信号通路图

PPAR Signaling Pathways

PPAR信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息(PMID)
ST-13 cells Function assay 5 μM 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
HepG2 cells Function assay 50 μM 24 h Induction of p53 protein level in human HepG2 cells at 50 uM up to 24 hrs by immunoblot analysis
HEK293 cells Function assay 10 μM 24 h Transactivation of PPAR-gamma transfected in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay
HepG2 cells Function assay 0.5-12.5 μM 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
HepG2 cells Function assay 0.5-12.5 μM 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
MA104 cells Cytotoxicity assay 24 h Cytotoxicity against monkey MA104 cells after 24 hrs, TD50=18.5 μM
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
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
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
LNCAP cells Cytotoxicity assay 24 h Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay, IC50=22 μM
PC3 cells Cytotoxicity assay 24 h Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50=30 μM
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
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
3T3-L1 cells Function assay Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.13 μM
PC12 cells Proliferation assay Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay, IC50=15 Μm
A549 Growth inhibition assay Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay, GI50=15 μM
3T3L1 cells Function assay Increase in 2-deoxyglucose uptake in mouse 3T3L1 cells at 3 uM by liquid scintillation counter
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
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
3T3L1 cells Function assay Agonist activity at PPARgamma in mouse 3T3L1 cells, EC50=1 μM
HepG2 cells Function assay Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of phosphoenolpyruvate carboxykinase mRNA by RT-PCR analysis
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
HepG2 cells Function assay Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of glucose-6-phosphatase mRNA by RT-PCR analysis
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
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
CV1 cells Function assay Transactivation of human PPARgamma expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.4 μM
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
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
点击查看更多细胞系数据

生物活性

产品描述 Troglitazone是PPAR的有效激动剂，PPAR是配体激活的转录因，可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。
靶点
Ferroptosis [6] PPAR [1]
体外研究(In Vitro)
体外研究活性

Troglitazone通过阻滞细胞周期和引起细胞凋亡性死亡，显著地抑制细胞生长。在FTC-133细胞中，下调CD97（新型去分化标记）的表面表达；在TPC-1和FTC-133细胞中，上调钠碘转运体NIS mRNA。Troglitazone作为PPARγ激动剂，诱导甲状腺癌细胞的抗增殖和重分化作用[1]。在人类前列腺癌细胞中，Troglitazone不依赖于PPARγ信号通路，诱导Erk磷酸化[2]。TGZ(Troglitazone)上调NOS，诱导p53通路，抑制胆固醇合成，诱导依赖于p21 cyclin的激酶抑制剂，具有抗氧化功能，以不依赖于PPARγ的机制激活ERK。TGZ还能通过转录和转录后调节，诱导Egr-1的表达，并增强含Egr-1共有序列的启动子的结合亲和力及反式激活活性，因而诱导其他抗肿瘤发生蛋白的生成[3]。
细胞实验 细胞系 甲状腺癌细胞TPC-1, FTC-133, FTC-236, FTC-238, XTC-1和ARO82-1细胞
浓度 5, 10, 20, 40 μM
孵育时间 0, 2, 4, 6天
方法

收集融合率达到85%-100%的细胞，将其以3-5×103个细胞/孔的密度接种于96孔板中，培养于200μL/孔的H5培养基中。37℃培养24小时后，用不同浓度的troglitazone对细胞进行处理，每天更换新的培养基。在处理后0,2,4,6天时，进行MTT增殖检测。将MTT（400 μg/mL）加入每孔，并孵育3小时。然后将其溶解于0.04 N HCl/iso-propanol/3% SDS， 孵育1小时。检测595 nm/620 nm的吸光值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot ASCT2 / GLS1 c-Myc 25872876
Growth inhibition assay Cell viability 25872876
体内研究(In Vivo)
体内研究活性

Troglitazone是一种有效的抗糖尿病药，以一种全新的机制发挥作用。但是，在它被广泛使用后的几年内，发现它对一些个体具有肝脏损伤、造成肝功能衰竭[5]。TGZ显著抑制携有HCT-116, MCF-7, PC-3癌细胞的免疫缺陷小鼠的肿瘤生长[3]。在实验性慢性胰腺炎模型中，Troglitazone能够减轻胰腺损伤和炎症反应[4]。
动物实验 Animal Models C57BL/6小鼠
Dosages 0.2% (with chow)
Administration 口服
  • https://pubmed.ncbi.nlm.nih.gov/15785241/
  • https://pubmed.ncbi.nlm.nih.gov/22448169/
  • https://pubmed.ncbi.nlm.nih.gov/12475986/
  • https://pubmed.ncbi.nlm.nih.gov/15743784/
  • https://pubmed.ncbi.nlm.nih.gov/17575588/
  • https://pubmed.ncbi.nlm.nih.gov/27842070/

化学信息&溶解度

分子量 441.54 分子式

C24H27NO5S
CAS号 97322-87-7 SDF Download Troglitazone SDF
Smiles CC1=C(C2=C(CCC(O2)(C)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4)C(=C1O)C)C
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 88 mg/mL ( (199.3 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 15 mg/mL (33.97 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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