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
CAS: 97322-87-7
产品质控
批次：
纯度：
99.47%
99.47
Troglitazone相关产品
相关信号通路图
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 |
|---|---|---|---|---|---|
| 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 | 19268587 |
| 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 | 25851939 |
| 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 | 22579484 |
| 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 | 22342624 | |
| 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 | 22342624 | |
| MA104 cells | Cytotoxicity assay | 24 h | Cytotoxicity against monkey MA104 cells after 24 hrs, TD50=18.5 μM | 22365411 | |
| 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 | |
| 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 | |
| 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 | |
| LNCAP cells | Cytotoxicity assay | 24 h | Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay, IC50=22 μM | 22546208 | |
| PC3 cells | Cytotoxicity assay | 24 h | Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50=30 μM | 22546208 | |
| 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 | |
| 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 | |
| 3T3-L1 cells | Function assay | Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.13 μM | 9599241 | ||
| PC12 cells | Proliferation assay | Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay, IC50=15 Μm | 15109648 | ||
| A549 | Growth inhibition assay | Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay, GI50=15 μM | 15454234 | ||
| 3T3L1 cells | Function assay | Increase in 2-deoxyglucose uptake in mouse 3T3L1 cells at 3 uM by liquid scintillation counter | 18477507 | ||
| 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 | ||
| 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 | ||
| 3T3L1 cells | Function assay | Agonist activity at PPARgamma in mouse 3T3L1 cells, EC50=1 μM | 21493073 | ||
| HepG2 cells | Function assay | Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of phosphoenolpyruvate carboxykinase mRNA by RT-PCR analysis | 22424300 | ||
| 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 cells | Function assay | Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of glucose-6-phosphatase mRNA by RT-PCR analysis | 22424300 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 | ||
| 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 |
|
| 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 | |
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 |
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 |
|
体内溶解度 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
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。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
Tags: buy Troglitazone | Troglitazone ic50 | Troglitazone price | Troglitazone cost | Troglitazone solubility dmso | Troglitazone purchase | Troglitazone manufacturer | Troglitazone research buy | Troglitazone order | Troglitazone mouse | Troglitazone chemical structure | Troglitazone mw | Troglitazone molecular weight | Troglitazone datasheet | Troglitazone supplier | Troglitazone in vitro | Troglitazone cell line | Troglitazone concentration | Troglitazone nmr
