Troglitazone
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Catalog No.GC15272
One-Click Copy Product Info
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Troglitazone is an orally active agonist of the peroxisome proliferator-activated receptor γ (PPARγ), with EC50 values of 550nM and 780nM for human and murine receptors, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 97322-87-7
Sample solution is provided at 25 µL, 10mM.
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Troglitazone is an orally active agonist of the peroxisome proliferator-activated receptor γ (PPARγ), with EC50 values of 550nM and 780nM for human and murine receptors, respectively[1]. PPARγ is a widely expressed ligand-regulated transcription factor that controls the expression of genes involved in inflammation, redox balance, neurotrophic factor production, insulin sensitivity, and lipid and glucose metabolism[2]. By activating PPARγ, Troglitazone improves insulin resistance and regulates glucose and lipid metabolism, making it commonly used for the treatment of type II diabetes[3].
In vitro, treatment of mitochondria isolated from rat liver with Troglitazone (10, 50μM) for 5min induced mitochondrial swelling[4]. Treatment of C4-2 cells with Troglitazone (45μM) for 72h induced G0/G1 phase cell cycle arrest and increased the proportion of cells in the subG0 phase and the level of DNA fragmentation[5]. Treatment of human bladder cancer T24 and EJ cells with Troglitazone (25, 50μM) for 24h increased the ratio of light chain 3 (LC3)-II to actin in a time- and concentration-dependent manner[6].
In vivo, oral administration of Troglitazone (200mg/kg/day) for 5 weeks to male Balb/c mice bearing MIA Paca2 xenograft tumors significantly suppressed tumor growth without a significant effect on mouse body weight[7]. A single intraperitoneal injection of Troglitazone (300mg/kg) in female BALB/c mice significantly increased plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels after 6h, and this treatment induced pericentral hepatocyte necrosis within 24h[8].
References:
[1] WILSON T M, BROWN P J, STERNBACH D D, et al. The PPARs: from orphan receptors to drug discovery[J]. Journal of Medicinal Chemistry, 2000, 43(4): 527-550.
[2] CAI W, YANG T, LIU H, et al. Peroxisome proliferator-activated receptor γ (PPARγ): A master gatekeeper in CNS injury and repair[J]. Progress in Neurobiology, 2018, 163: 27-58.
[3] PLOSKER G L, FAULDS D. Troglitazone: a review of its use in the management of type 2 diabetes mellitus[J]. Drugs, 1999, 57(3): 409-438.
[4] OKUDA T, NORIOKA M, SHITARA Y, et al. Multiple mechanisms underlying troglitazone-induced mitochondrial permeability transition[J]. Toxicology and Applied Pharmacology, 2010, 248(3): 242-248.
[5] AKINYEKE T O, STEWART L V. Troglitazone suppresses c-Myc levels in human prostate cancer cells via a PPARγ-independent mechanism[J]. Cancer Biology & Therapy, 2011, 11(12): 1046-1058.
[6] YAN S, YANG X, CHEN T, et al. The PPARγ agonist Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells[J]. Cancer Gene Therapy, 2014, 21(5): 188-193.
[7] FUJITA M, HASEGAWA A, YAMAMORI M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer[J]. Journal of Experimental & Clinical Cancer Research, 2017, 36(1): 91.
[8] JIA R, ODA S, TSUNEYAMA K, et al. Establishment of a mouse model of troglitazone-induced liver injury and analysis of its hepatotoxic mechanism[J]. Journal of Applied Toxicology, 2019, 39(11): 1541-1556.
| Cell experiment [1]: | |
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Cell lines |
C4-2 cells (human prostate cancer cell lines) |
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Preparation Method |
Cells were treated with Troglitazone 45μM for 72h, the percentage of cells within the different phases of the cell cycle was determined using flow cytometry, and the level of DNA fragmentation was measured using a Cell Death ELISA. |
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Reaction Conditions |
45μM; 72h |
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Applications |
Troglitazone treatment induced G0/G1 phase cell cycle arrest and increased the proportion of subG0 phase cells and DNA fragmentation levels. |
| Animal experiment [2]: | |
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Animal models |
Balb/c male mice bearing MIA Paca2 xenografts |
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Preparation Method |
Balb/c male mice were subcutaneously inoculated in the back with MIA Paca2 cells (5 × 106 cells) 14 days before the start of Troglitazone administration. Mice were then orally administered 200mg/kg of Troglitazone daily for 5 weeks. Tumor volume was measured bi-dimensionally and volume was calculated by the formula (length × width2) × 0.5, and mouse body weights were monitored throughout the experiment. |
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Dosage form |
200mg/kg/day; 5 weeks; p.o. |
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Applications |
Troglitazone exhibited inhibitory effects on tumor growth in the MIA Paca2 xenograft model, the body weights of mice were not affected compared to those of the vehicle administration group. |
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References: |
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| Cas No. | 97322-87-7 | SDF | |
| Chemical Name | 5-[[4-[(6-hydroxy-2,5,7,8-tetramethyl-3,4-dihydrochromen-2-yl)methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | CC1=C(C(=C2CCC(OC2=C1C)(C)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4)C)O | ||
| Formula | C24H27NO5S | M.Wt | 441.54 |
| Solubility | ≥ 20.9 mg/mL in DMSO, ≥ 3.34 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2648 mL | 11.324 mL | 22.648 mL |
| 5 mM | 453 μL | 2.2648 mL | 4.5296 mL |
| 10 mM | 226.5 μL | 1.1324 mL | 2.2648 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >96.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)