CITCO is a potent, selective agonist of orphan nuclear constitutive androstane receptor (CAR) with EC50 of 49 nM (human CAR) in CAR/SRC-1 FRET assays.
CITCO displayed calculated EC50 values of 25 nm in the CAR transient transfection assay, >100-fold selectivity over PXR, did not have any detectable activity on a panel of 15 nuclear receptors.
CITCO promotes nuclear translocation of humanCAR.
CITCO shows robust effects on CAR target genes CYP2B expression in mouse versushuman cells.
