Home Metabolism PPAR agonist - Autophagy activator - Apoptosis related activator - Ferroptosis inhibitor Troglitazone For research use only.

Troglitazone

Synonyms: CS-045, Romglizone

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.

Troglitazone Chemical Structure

Troglitazone Chemical Structure

CAS: 97322-87-7

Selleck's Troglitazone has been cited by 3 publications

Purity & Quality Control

Batch: S843201 DMSO] 88 mg/mL] false] Ethanol] 15 mg/mL] false] Water] Insoluble] false Purity: 99.47%
99.47

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
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
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
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
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
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 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
3T3L1 cells Function assay Agonist activity at PPARgamma in mouse 3T3L1 cells, EC50=1 μM 21493073
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
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
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
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
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
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Biological Activity

Description Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
Targets
Ferroptosis [6] PPAR [1]
In vitro
In vitro

Troglitazone significantly inhibits cell growth by cell cycle arrest and apoptotic cell death. Troglitazone also downregulates surface expression of CD97, a novel dedifferentiation marker, in FTC-133 cells and upregulated sodium iodide symporter (NIS) mRNA in TPC-1 and FTC-133 cells. Troglitazone, a PPARγ agonist, induces antiproliferation and redifferentiation in thyroid cancer cell lines[1]. Troglitazone induces Erk phosphorylation in human prostate cancer cells via a PPARγ-independent signaling pathway[2]. TGZ(Troglitazone) up-regulates nitric oxide synthesis, induces the p53 pathway, inhibits cholesterol biosynthesis, induces p21 cyclin-dependent kinase inhibitor, has antioxidant function, and activates extracellular signal-regulated protein kinase (ERK) in a PPARγ-independent manner. TGZ induces Egr-1 expression by transcriptional and post-transcriptional regulation. Egr-1 induction by TGZ results in the increase of binding affinity and transactivation of the promoter containing Egr-1 consensus sequences, thereby possibly inducing other anti-tumorigenic proteins[3].
Cell Research Cell lines Thyroid cancer cell lines TPC-1, FTC-133, FTC-236, FTC-238, XTC-1 and ARO82-1 cell lines
Concentrations 5, 10, 20, 40 μM
Incubation Time 0, 2, 4, and 6 days
Method

Growth experiments are done in a 96-well plate in hexaplicate. Cells at 85%-100% confluency are harvested with 1×Trypsin/EDTA solution and seeded into a 96-well plate at 3-5×103 cells per well depending upon growth rate and maintained in 200 μL H5 medium in a humidified incubator. After 24 hours, cells are incubated with different concentrations of troglitazone and the media was changed daily. Colorometric dimethyl-thiazol-diphenyltetrazolium bromide (MTT) proliferation assays are performed at 0, 2, 4, and 6 days after treatment. MTT (400 μg/mL) is added to each well and incubated for 3 hours. It is solubilized with 0.04 N HCl/iso-propanol/3% SDS and incubated for 1 hour. The optical densities in the 96-well plates are determined using an enzyme-linked immunosorbent assay (ELISA) microplate reader at 595 nm/620 nm.
Experimental Result Images Methods Biomarkers Images PMID
Western blot ASCT2 / GLS1 c-Myc 25872876
Growth inhibition assay Cell viability 25872876
In Vivo
In vivo

Troglitazone is an effective antidiabetic drug with a fundamentally new mechanism of action. However, within a year after its widespread use, individual cases of liver injury and failure are reported[5]. TGZ significantly inhibits tumor growth of human colorectal cancer cells (HCT-116), human breast cancer cells (MCF-7), and human prostate cancer cells (PC-3) in immunodeficient mice[3]. Troglitazone attenuates pancreatic damage and inflammation in experimental chronic pancreatitis[4].
Animal Research Animal Models C57BL/6 mice
Dosages 0.2% (with chow)
Administration oral administration

Chemical lnformation & Solubility

Molecular Weight 441.54 Formula

C24H27NO5S
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (199.3 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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