Chemical Name: 6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichlorobenzyl)oxime
Biological ActivityConstitutive 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes.
Maglich et al.
A single amino acid controls the functional switch of human CAR1 to the xenobiotic sensitive splicing variant CAR3.
Clen et al.
Constitutive androstane receptor-vitamin D receptor crosstalk: consequence on CYP24 gene expression.
Moreau et al.
Citations for CITCO
The citations listed below are publications that use Tocris products. Selected citations for CITCO include:
3 Citations: Showing 1 - 3
Constitutive androstane receptor 1 is constitutively bound to chromatin and 'primed' for transactivation in hepatocytes.
Authors: McMahon Et al.
Mol Pharmacol 2019;95:97
CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor.
Authors: Cherian Et al.
Mol Pharmacol 2015;87:878
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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