Troglitazone
Peroxisome proliferator-activated receptor gamma (PPARγ) agonists and PPARg/a dual agonists are used in the treatment of type 2 diabetes mellitus. Troglitazone is a prototypical sarcomagenic PPARg agonist.
In vitro: Troglitazone PPARγ ligands showed potent inhibitory effect on proliferation, and could induce RCC cell apoptosis, suggesting that the PPARγ ligands have potential antitumor effects on renal carcinoma cells [1].
In vivo: Troglitazone increased EC proliferation in brown and white adipose tissue and liver in mice at sarcomagenic doses (400 and 800 mg/kg) after four weeks of treatment [2].
Clinical trial: Several clinical trials have been conducted to investigate the efficacy, safety and pharmacokinetics of troglitazone in the liposarcoma and diabtes mellitus patients [3].
References:
[1] Yang FG, Zhang ZW, Xin DQ, Shi CJ, Wu JP, Guo YL, Guan YF. Peroxisome proliferator-activated receptor gamma ligands induce cell cycle arrest and apoptosis in human renal carcinoma cell lines. Acta Pharmacol Sin. 2005;26(6):753-61.
[2] Kakiuchi-Kiyota S, Arnold LL, Yokohira M, Koza-Taylor P, Suzuki S, Varney M, Pennington KL, Cohen SM. Evaluation of direct and indirect effects of the PPARγ agonist troglitazone on mouse endothelial cell proliferation. Toxicol Pathol. 2011;39(7):1032-45.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 441.54 |
| Cas No. | 97322-87-7 |
| Formula | C24H27NO5S |
| Synonyms | Rezulin;CS-045;Noscal |
| Solubility | insoluble in H2O; ≥20.9 mg/mL in DMSO; ≥3.34 mg/mL in EtOH with gentle warming and ultrasonic |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(C(=C2CCC(OC2=C1C)(C)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4)C)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | Troglitazone(CS-045) is a agonist of PPARγ. | |||||
| Targets | PPARγ | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
