| 货号 | 16027-5mg |
| 描述 | The constitutive androstane receptor (CAR) is a nuclear receptor that functions as a sensor of toxic compounds and enhances their elimination.1 CITCO is an agonist of human CAR (EC50 = 49 nM).2 It induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes, including several cytochrome P450 isoforms.2 CITCO less potently activates human pregnane X receptor (EC50 = 3 µM) and has no detectable activity on other nuclear receptors at 10 µM.2 It is selective for human CAR, whereas TCPOBOP (Item No. 14140) is selective for mouse CAR.1 CITCO does activate alternative splice variants of human CAR that are also found in liver cells.3 It is commonly used to study the action of human CAR in hepatocytes.4,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Timsit, Y.E. and Negishi, M. CAR and PXR: The xenobiotic-sensing receptors. Steroids 72(3), 231-246 (2007). 2.Maglich, J.M.,Parks, D.J.,Moore, L.B., et al. Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. The Journal of Biological Chemisty 278(19), 17277-17283 (2003). 3.Jinno, H.,Tanaka-Kagawa, T.,Hanioka, N., et al. Identification of novel alternative splice variants of human constitutive androstane receptor and characterization of their expression in the liver. Molecular Pharmacology 65(3), 496-502 (2004). 4.Kanno, Y.,Tanuma, N.,Yatsu, T., et al. Nigramide J is a novel potent inverse agonist of the human constitutive androstane receptor. Pharmacol.Res.Perspect. 2(1), 1-8 (2014). 5.Chen, T.,Laurenzana, E.M.,Coslo, D.M., et al. Proteasomal interaction as a critical activity modulator of the human constitutive androstane receptor. Biochemistry Journal 458(1), 95-107 (2014). | |
| 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 | 436.7 |
| 分子式 | C19H12Cl3N3OS |
| CAS号 | 338404-52-7 |
| 稳定性 | ≥ 2 years |
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