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Troglitazone

Catalog No. T3170   CAS 97322-87-7
Synonyms: CS-045, Romozin, Rezulin, Romglizone, Noscal, Prelay

Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

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Troglitazone Chemical Structure
Troglitazone, CAS 97322-87-7
Pack Size Availability Price/USD Quantity
2 mg In stock $ 35.00
5 mg In stock $ 56.00
10 mg In stock $ 90.00
25 mg In stock $ 175.00
50 mg In stock $ 322.00
100 mg In stock $ 588.00
500 mg In stock $ 1,230.00
1 mL * 10 mM (in DMSO) In stock $ 77.00
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Purity: 99.62%
Purity: 99.36%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.
Targets&IC50 PPARγ (human):550 nM (EC50), PPARγ (murine):780 nM (EC50)
In vitro Troglitazone inhibits the growth of 786-O and A498 cells with EC50 values of 5.71 μM and 8.38 μM. Troglitazone(5 μM) significantly inhibits the CYP2C8-dependent paclitaxel 6a-hydroxylation and CYP2C9-dependent S-warfarin 7-hydroxylation. Troglitazone extensively suppresses CYP2C19-dependent S-mephenytoin 4′-hydroxylation and CYP3A4-dependent testosterone 6b-hydroxylation and moderately influences the CYP1A2- and CYP2B6-dependent 7-ethoxycoumarin O-deethylation, CYP2A6-dependent coumarin 7-hydroxylation and CYP2D6-dependent bufuralol 1′-hydroxylation. CYP2E1-dependent 7-ethoxycoumarin O-deethylation is not inhibited.
In vivo Local hypoxia is observed in liver but not in adipose tissue in troglitazone-treated mice. A significant increase in Ki-67/CD31 LI in liver, BAT, and WAT is observed in the 400 mg/kg troglitazone group. Troglitazone reduces the incidence of diabetes by 16 weeks compared to controls, when administered by gavage from weaning at a dose of 400 mg/kg body weight.
Kinase Assay Standard incubation mixtures (final volume of 0.20 mL) containe recombinant P450 (0.010 μM) in 50 mM potassium phosphate bu?er (pH 7.4) containing an NADPH-generating system (0.5 mm NADP+, 5 mM glucose 6-phosphate, 0.5 unit glucose 6-phosphate dehydrogenase/mL) and substrates (1±100 lM). For determination of CYP1A2, CYP2B6, CYP2E1 and CYP3A4 activities, 100 mM potassium phosphate buffer (pH 7.4) is used. When human liver microsomes are used as the enzyme source, 500, 25, 100 and 25 pmol totalP450 per mL are used for paclitaxel 6a-hydroxylation, S-warfarin 7-hydroxylation,S-mephenytoin 4′-hydroxylation and testosterone 6b-hydroxylation respectively.
Cell Research Troglitazone is made at 100 mM concentration in DMSO and added to the culture medium at the final concentration of less than 0.1%. The effect of PPARγ ligands on cell proliferation of RCC cells is determined using MTT assay. Briefly, cells of 0.5×l04 cells/well are inoculated into a 96-well plate, treated with pioglitazone or troglitazone at various concentrations. After an incubation for 24 h, 20 μL/well 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT, 5 g/L) is added to each well, the medium is then removed, and 200 μL of 0.04mol/LHCl in isopropanol is added to dissolve the reduced formazan product. The plate is read in a microplate reader at 590 nm.
Synonyms CS-045, Romozin, Rezulin, Romglizone, Noscal, Prelay
Molecular Weight 441.54
Formula C24H27NO5S
CAS No. 97322-87-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 4.4 mg/mL (10 mM)), Heating is recommended.

DMSO: 44.2 mg/mL (100 mM)

TargetMolReferences and Literature

1. Park JW, et al. Thyroid. 2005, 15(3):222-31. 2. Bolden A, et al. PPAR Res. 2012, 2012:929052. 3. Baek SJ, et al. J Biol Chem. 2003, 278(8):5845-53. 4. van Westerloo DJ, et al. Am J Pathol. 2005, 166(3):721-8. 5. Jaeschke H. Toxicol Sci. 2007, 97(1):1-3. 6. 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. 7. 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.

TargetMolCitations

1. Kazberuk A, Chalecka M, Palka J, et al. Nonsteroidal Anti-Inflammatory Drugs as PPARγ Agonists Can Induce PRODH/POX-Dependent Apoptosis in Breast Cancer Cells: New Alternative Pathway in NSAID-Induced Apoptosis. International Journal of Molecular Sciences. 2022, 23(3): 1510. 2. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989. 3. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Diabetic Compound Library Anti-Pancreatic Cancer Compound Library Nuclear Receptor Compound Library Drug-induced Liver Injury (DILI) Compound Library

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Keywords

Troglitazone 97322-87-7 Apoptosis Autophagy DNA Damage/DNA Repair Metabolism Ferroptosis PPAR Peroxisome proliferator-activated receptors CS-045 Inhibitor Romozin Rezulin Romglizone Noscal CS 045 CS045 inhibit Prelay inhibitor

 

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