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Troglitazone (CS-045)

Cat. No. M5171
Troglitazone (CS-045) Structure
Synonym:

Rezulin, Romglizone, Prelay, CS-045, CS045, CS 045, Romozin

Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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. Troglitazone induces Erk phosphorylation in human prostate cancer cells via a PPARγ-independent signaling pathway. 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. 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. 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. Troglitazone attenuates pancreatic damage and inflammation in experimental chronic pancreatitis.

Protocol
Cell Experiment
Cell lines Thyroid cancer cell lines TPC-1, FTC-133, FTC-236, FTC-238, XTC-1 and ARO82-1 cell lines
Preparation 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.
Concentrations 5, 10, 20, 40 μM
Incubation time 0, 2, 4, and 6 days
Animal Experiment
Animal models C57BL/6 mice
Formulation
Dosages 0.2% (with chow)
Administration oral administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 441.54
Formula C24H27NO5S
CAS Number 97322-87-7
Purity >99%
Solubility 88 mg/mL in DMSO
Storage at -20°C
References

Cancer drug troglitazone stimulates the growth and response of renal cells to hypoxia inducible factors.
Taub M Biochem Biophys Res Commun. 2016 Mar 11;471(3):342-7. PMID: 26869517.

Troglitazone Stimulates Cancer Cell Uptake of 18F-FDG by Suppressing Mitochondrial Respiration and Augments Sensitivity to Glucose Restriction.
Moon SH, et al. J Nucl Med. 2016 Jan;57(1):129-35. PMID: 26449833.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Troglitazone (CS-045), Rezulin, Romglizone, Prelay, CS-045, CS045, CS 045, Romozin supplier, PPAR, inhibitors

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