货号 | 10011286-1g |
描述 | Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1 They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3 Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hyperlipidemia, and atherosclerosis. Chenodeoxycholic acid (CDCA) is a hydrophobic primary bile acid that activates nuclear receptors involved in cholesterol metabolism.3,4EC50 concentrations for activation of FXR range from 13-34 μM.5,6 In cells, CDCA also binds to bile acid binding proteins (BABP) with a reported stoichiometry of 1:2.4 CDCA toxicity is linked to increased cellular glutathione levels and increased oxidative stress. Exposure of cells to excess CDCA contributes to liver and intestinal cancers.3 |
别名 | Anthropodeoxycholic Acid;CDCA;Fluibil;Hekbilin;Kebilis;Ulmenide; |
供应商 | Cayman |
应用文献 | |
1.Makishima, M.,Okamoto, A.Y.,Repa, J.J., et al. Identification of a nuclear receptor for bile acids. Science 284, 1362-1365 (1999). 2.Barbier, O.,Torra, I.P.,Sirvent, A., et al. FXR induces the UGT2B4 enzyme in hepatocytes: A potential mechanism of negative feedback control of FXR activity. Gastroenterology 124, 1926-1940 (2003). 3.Tan, K.P.,Yang, M. and Ito, S. Activation of nuclear factor (erythroid-2 like) factor 2 by toxic bile acids provokes adaptive defense responses to enhance cell survival at the emergence of oxidative stress. Molecular Pharmacology 72(5), 1380-1390 (2007). 4.Eliseo, T.,Ragona, L.,Catalano, M., et al. Structural and dynamic determinants of ligand binding in the ternary complex of chicken liver bile acid binding protein with two bile salts revealed by NMR. Biochemistry 46(44), 12557-12567 (2007). 5.Urizar, N.L.,Liverman, A.B.,Dodds, D.T., et al. A natural product that lowers cholesterol as an anatagonist ligand for FXR. Science 296, 1703-1706 (2002). 6.Glickman, J.F.,Wu, X.,Mercuri, R., et al. A comparison of ALPHAScreen, TR-FRET, and TRF as assay methods for FXR nuclear receptors. Journal of Biomolecular Screening 7(1), 3-10 (2002). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 392.6 |
分子式 | C24H40O4 |
CAS号 | 474-25-9 |
稳定性 | ≥ 2 years |
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