Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday.
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Please feel free to continue placing orders via our website or via fax at 734-971-3640. You may send an email to customer service at custserv@caymanchem.com , or to technical support at techserv@caymanchem.com which we will respond to the next business day. Cayman will resume regular business hours and shipping schedules on Tuesday, May 29, 2012. Thank you for your patience and understanding.
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
Copy SMILES to clipboard
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: