Troglitazone-d4 是氘标记的曲格列酮。 Troglitazone 是一种 PPARγ 激动剂，对人和鼠 PPARγ 受体的 EC50 分别为 550 nM 和 780 nM。
Troglitazone-d4 is intended for use as an internal standard for the quantification of troglitazone by GC- or LC-MS. Troglitazone is a selective agonist of peroxisome proliferator-activated receptor γ (PPARγ; EC50s = 0.78 and 0.55 μM for the mouse and human receptors, respectively, in a transactivation assay).1 It is selective for PPARγ over PPARα and PPARδ, at which it is inactive at concentrations up to 10 μM. Troglitazone (500 mg/kg twice per day) exhibits antihyperglycemic and antihyperlipidemic properties in Zucker diabetic fatty rats, reducing plasma glucose and triglyceride levels by 61 and 87%, respectively.2 It also induces cell cycle arrest at the G1 phase in SK-HEP-1 and Hep3B hepatocellular carcinoma cells when used at a concentration of 10 μM and increases apoptosis in these cells at concentrations of 30 μM and higher.3
|1. Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J. Med. Chem. 43(4), 527-550 (2000).|2. Henke, B.R., Blanchard, S.G., Brackeen, M.F., et al. N-(2-Benzoylphenyl)-L-tyrosine PPARγ agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. J. Med. Chem. 41(25), 5020-5036 (1998).|3. Yoshizawa, K., Cioca, D.P., Kawa, S., et al. Peroxisome proliferator-activated receptor γ ligand troglitazone induces cell cycle arrest and apoptosis of hepatocellular carcinoma cell lines. Cancer 95(10), 2243-2251 (2002).
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