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Troglitazone

MCE China：Troglitazone

Brand：MedChemExpress (MCE)

Cat. No.HY-50935

CAS：97322-87-7

Synonyms：CS-045

Purity：99.78%

Storage：Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.

In Vitro：Troglitazone (2-200 μM, 24 h) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 and PANC-1 cells), with IC50s of 49.9±1.2 and 51.3±5.3 μM, respectively[2]. Troglitazone (50 μM, 24 h) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression[2]. Troglitazone (0-4 μM, 12 h) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells (A549, HCC-15 and Calu-3)[3]. Troglitazone (0-4 μM, 12 h) induces autophagy and sensitized apoptosis mediated by TRAIL in A549 cells[1].

In Vivo：Troglitazone (200 mg/kg, p.o., every day for 5 weeks) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model[2].

Animal Administration：Balb/c male mice (4 weeks old) are subcutaneously inoculated in the back with MIA Paca2 cells (5 × 106 cells/100 μL in PBS) 14 days prior to starting Troglitazone administration. Mice are then orally administered 200 mg/kg Troglitazone in 0.5% methylcellulose solution or vehicle daily for 5 weeks. Tumor size is measured bi-dimensionally and the volume is calculated using the formula (length × width2) × 0.5. Body weights of mice are also monitored throughout the experiment[2].

Cell Assay：Briefly, cells are seeded into 96-well plates at a density of 1 × 105 cells/well and incubated for 24 h. The cells are treated with Troglitazone in the presence or absence of other chemicals for a further 24 h using FBS-free medium. The assay utilizes the conversion of alamar blue reagent to fluorescent resorufin by metabolically active cells. The resorufin signal is measured at an excitation wavelength of 530 nm and an emission wavelength of 580 nm. The 50% growth inhibitory concentrations (IC50) are calculated according to the sigmoid inhibitory effect model E = IC50 γ/(IC50 γ + Cγ), where E represents the surviving fraction (% of control), C represents the drug concentration in the medium, and γ represents the Hill coefficient. For co-exposure studies, the Troglitazone dosage is set to approximately the IC50 value for each cell line[2].

IC50 & Target：PPARγ 550 nM (EC50, Human PPARγ)

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References：

[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.  [Content Brief]

[2]. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91.  [Content Brief]

[3]. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831.  [Content Brief]

[4]. Knowler WC, et al. Prevention of type 2 diabetes with troglitazone in the Diabetes Prevention Program. Diabetes. 2005 Apr;54(4):1150-6.  [Content Brief]