| 货号 | 14140-5mg |
| 描述 | The mouse constitutive androstane receptor (mCAR), with the retinoid X receptor, binds to the retinoic acid response element to upregulate the expression of proteins that metabolize xenobiotics.1 TCPOBOP is an agonist for mCAR (EC50 = 20 nM) that is effective for the mouse receptor but not for human or rat CAR receptors.2,3 Through its effects on mCAR, TCPOBOP potently induces cytochrome P450 monooxygenases and multidrug resistance and xenobiotic efflux proteins.4,5,6 The action of TCPOBOP on mCAR-mediated gene expression can be repressed by retinoic acids.7 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Choi, H.S.,Chung, M.,Tzameli, I., et al. Differential transactivation by two isoforms of the orphan nuclear hormone receptor CAR. The Journal of Biological Chemisty 272(38), 23565-23571 (1997). 2.Tzameli, I.,Pissios, P.,Schuetz, E.G., et al. The xenobiotic compound 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene is an agonist ligand for the nuclear receptor CAR. Molecular and Cellular Biology 20(9), 2951-2958 (2000). 3.Timsit, Y.E. and Negishi, M. CAR and PXR: The xenobiotic-sensing receptors. Steroids 72(3), 231-246 (2007). 4.Smith, G.,Henderson, C.J.,Parker, M.G., et al. 1,4-Bis[2-(3,5-dichloropyridyloxy)]benzene, an extremely potent modulator of mouse hepatic cytochrome P-450 gene expression. Biochemistry Journal 289(Pt 3), 807-813 (1993). 5.Wang, X.,Sykes, D.B. and Miller, D.S. Constitutive androstane receptor-mediated up-regulation of ATP-driven xenobiotic efflux transporters at the blood-brain barrier. Molecular Pharmacology 78(3), 376-383 (2010). 6.Maher, J.M.,Cheng, X.,Slitt, A.L., et al. Induction of the multidrug resistance-associated protein family of transporters by chemical activators of receptor-mediated pathways in mouse liver. Drug Metabolism and Disposition 33(7), 956-962 (2005). 7.Kakizaki, S.,Karami, S. and Negishi, M. Retinoic acids repress constitutive active receptor-mediated induction by 1,4-bis[2-(3,5-dichloropyridyloxy)]benzene of the CYP2B10 gene in mouse primary hepatocytes. Drug Metabolism and Disposition 30(2), 208-211 (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 | 402.1 |
| 分子式 | C16H8Cl4N2O2 |
| CAS号 | 76150-91-9 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |