CITCO (CAS 338404-52-7)
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CITCO is a cell-permeable imidazothiazole compound that acts as a potent and selective agonist for the human MB67 (orphan nuclear constitutive androstane receptor, CAR). CITCO also displays ~100-fold greater selectivity for MB67 (CAR) over xenobiotic pregnane X receptor (PXR) in transient transfection assays (EC50 = 25 nM vs. 3 muM) and shows no detectable activity on 15 other nuclear receptors tested even at concentrations as high as 10 muM. Citco, or 2-chloro-4-nitroaniline, is a yellow crystalline solid employed in laboratory experiments due to its diverse properties. With a melting point of 160° C and a boiling point of 238° C, Citco acts as an inhibitor for specific enzymes in the body, including cytochrome P450 enzymes.
CITCO (CAS 338404-52-7) References
- Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. | Maglich, JM., et al. 2003. J Biol Chem. 278: 17277-83. PMID: 12611900
- Transcriptional regulation of cytochrome p450 2B genes by nuclear receptors. | Wang, H. and Negishi, M. 2003. Curr Drug Metab. 4: 515-25. PMID: 14683479
- Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells. | Chakraborty, S., et al. 2011. Br J Cancer. 104: 448-59. PMID: 21224854
- New in vitro tools to study human constitutive androstane receptor (CAR) biology: discovery and comparison of human CAR inverse agonists. | Küblbeck, J., et al. 2011. Mol Pharm. 8: 2424-33. PMID: 22044162
- TO901317, a potent LXR agonist, is an inverse agonist of CAR. | Kanno, Y., et al. 2013. J Toxicol Sci. 38: 309-15. PMID: 23665929
- Nigramide J is a novel potent inverse agonist of the human constitutive androstane receptor. | Kanno, Y., et al. 2014. Pharmacol Res Perspect. 2: 2. PMID: 25505573
- The Use of the LanthaScreen TR-FRET CAR Coactivator Assay in the Characterization of Constitutive Androstane Receptor (CAR) Inverse Agonists. | Carazo, A. and Pávek, P. 2015. Sensors (Basel). 15: 9265-76. PMID: 25905697
- Quantitative high-throughput identification of drugs as modulators of human constitutive androstane receptor. | Lynch, C., et al. 2015. Sci Rep. 5: 10405. PMID: 25993555
- Activation of the Constitutive Androstane Receptor Increases the Therapeutic Index of CHOP in Lymphoma Treatment. | Hedrich, WD., et al. 2016. Mol Cancer Ther. 15: 392-401. PMID: 26823489
- Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies. | Liang, D., et al. 2019. Eur J Med Chem. 179: 84-99. PMID: 31247375
- DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor. | Liang, D., et al. 2019. ACS Med Chem Lett. 10: 1039-1044. PMID: 31312405
- CITCO Directly Binds to and Activates Human Pregnane X Receptor. | Lin, W., et al. 2020. Mol Pharmacol. 97: 180-190. PMID: 31882411
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CITCO, 5 mg | sc-202544 | 5 mg | $84.00 | |||
CITCO, 25 mg | sc-202544A | 25 mg | $312.00 |