CITCO
Chemical Name: 6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl)oxime
Purity: ≥98%
Biological Activity
CITCO is a constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). Displays > 100-fold selectivity over PXR receptors and no activity at LXR, ERα, ERβ, PPAR, RAR, FXR, VDR and THR. Induces CAR nuclear translocation and expression of CYP2B6 in hepatocytes in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Triclocarban Mediates Induction of Xenobiotic Metabolism through Activation of the Constitutive Androstane Receptor and the Estrogen Receptor Alpha.
Yueh MF, Li T, Evans RM, Hammock B, Tukey RH
PLoS ONE, 2012;7(6):e37705. -
Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes.
Maglich et al.
J.Biol.Chem., 2003;278:17277 -
A single amino acid controls the functional switch of human CAR1 to the xenobiotic sensitive splicing variant CAR3.
Clen et al.
J.Pharmacol.Exp.Ther., 2009;332:106
Product Datasheets
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Citations for CITCO
The citations listed below are publications that use Tocris products. Selected citations for CITCO include:
4 Citations: Showing 1 - 4
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(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells.
Authors: Petr Et al.
Front Pharmacol 2021;12:713149
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Constitutive androstane receptor 1 is constitutively bound to chromatin and 'primed' for transactivation in hepatocytes.
Authors: McMahon Et al.
Mol Pharmacol 2019;95:97
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CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor.
Authors: Cherian Et al.
Mol Pharmacol 2015;87:878
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Triclocarban mediates induction of xenobiotic metabolism through activation of the constitutive androstane receptor and the estrogen receptor alpha.
Authors: Yueh Et al.
PLoS One 2012;7:e37705
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