Constitutive androstane receptor (CAR) agonist (EC50
= 49 nM). Displays > 100-fold selectivity over PXR receptors and no activity at LXR, ERα
, PPAR, RAR, FXR, VDR and THR. Induces CAR nuclear translocation and expression of CYP2B6 in hepatocytes in vitro
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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.