CITCO is a novel potent and selective agonist for the human orphan nuclear receptor CAR (constitutive androstane receptor). CITCO displayed an EC50 of 49 nM in a CAR FRET assay and showed 50-fold selectivity for CAR over PXR. CITCO displayed no activity against a panel of 15 other nuclear receptors at a concentration of 10 µM. In hepatocytes CITCO induced CAR nuclear translocation and induced the CAR target gene CYP2B6.
Product Details
| Alternative Name: | 6-(4-Chlorophenyl)imidazo[2,1-b] [1,3]thiazole-5-carbaldehyde O-3,4-dichlorobenzyl) oxime |
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| Formula: | C19H12Cl3N3OS |
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| MW: | 436.7 |
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| CAS: | 338404-52-7 |
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| Appearance: | Pale orange solid. |
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| Solubility: | Soluble in DMF (25mg/ml) or DMSO (10mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Development and Experimental Validation of Regularized Machine Learning Models Detecting New, Structurally Distinct Activators of PXR: S. Hirte, et al.; Cells
11, 1253 (2022),
Abstract;
Activating and Inhibitory Functions of WNT/β-catenin in the Induction of Cytochromes P450 by Nuclear Receptors in HepaRG Cells: M. Thomas, et al.; Mol. Pharmacol. (2015),
Application(s): Cell Culture,
Abstract;
Full Text
Comparative Analysis and Functional Characterization of HC-AFW1 Hepatocarcinoma Cells: CYP Expression and Induction by Nuclear Receptor Agonists: A. Braeuning, et al.; Drug Metab. Dispos.
43, 1781 (2015),
Application(s): Cell Culture,
Abstract;
Full Text
Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes: J.M. Maglich, et al.; J. Biol. Chem.
278, 17277 (2003),
Abstract;
Full Text
