CITCO

BML-GR233

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Constitutive androstane receptor ligand

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.

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Product Details

Alternative Name	6-(4-Chlorophenyl)imidazo[2,1-b] [1,3]thiazole-5-carbaldehyde O-3,4-dichlorobenzyl) oxime
Appearance	Pale orange solid.
CAS	338404-52-7
Couple Target	Constitutive androstane receptor
Couple Type	Ligand
Formula	C₁₉H₁₂Cl₃N₃OS
MW	436.7
Solubility	Soluble in DMF (25mg/ml) or DMSO (10mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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
Indirect activation of the SV23 and SV24 splice variants of human constitutive androstane receptor: analysis with 3-hydroxyflavone and its analogues: Lau, A. J., Chang, T. K., et al.; Br. J. Pharmacol. 170, 403 (2013), Abstract
Effects of atorvastatin metabolites on induction of drug-metabolizing enzymes and membrane transporters through human pregnane X receptor: Hoffart, E., Ghebreghiorghis, L., et al.; Br. J. Pharmacol. 165, 1595 (2012), Abstract
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

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CITCO

BML-GR233

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