CITCO

CITCO is an agonist of human CAR (EC₅₀ = 49 nM).¹ It induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes, including several cytochrome P450 isoforms.¹ CITCO less potently activates human pregnane X receptor (EC₅₀ = 3 µM) and has no detectable activity on other nuclear receptors at 10 µM.¹ It is selective for human CAR, whereas TCPOBOP (Item No. 14140) is selective for mouse CAR.² 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

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1. 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).

2. Timsit, Y.E., and Negishi, M. CAR and PXR: The xenobiotic-sensing receptors. Steroids 72(3), 231-246 (2007).

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. Mol. Pharmacol. 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), 2 (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. Biochem. J. 458(1), 95-107 (2014).