The aryl hydrocarbon receptor (AhR) is a ligand-dependent intracellular transcription factor whose ligands include some of the most infamous xenobiotics, including dioxin (TCDD, 2,3,7,8-tetrachlorodibenzoparadioxin), benzo[a]pyrene, and numerous polyaromatic hydrocarbons from soot particles and coal tar.1 CAY10464 is a potent and selective AhR antagonist, with a Ki of 1.4 nM when tested in rabbit liver cytosol preparations.2 It is inactive as an estrogen receptor ligand even at 100 µM.
1
Denison, M.S., and Nagy, S.R. Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals.. Annu Rev Pharmacol Toxicol43309-334(2003).
2
de Medina, P., Casper, R., Savouret, J., et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. J Med Chem48287-291(2005).
Room temperature
in continental US; may vary elsewhere
SMILES
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COc1ccc(cc1)\C=C/c1cc(Cl)cc(Cl)c1
Background Reading
de Medina, P., Casper, R., Savouret, J., et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. J Med Chem48287-291(2005).
Denison, M.S., and Nagy, S.R. Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals.. Annu Rev Pharmacol Toxicol43309-334(2003).
CAY10464 is available in the following screening
library: