A resveratrol-based aryl hydrocarbon receptor agonist
CAY 10465 is a selective and high-affinity AhR agonist, with a Ki of 0.2 nM, and shows no effect on estrogen receptor (Ki >100000 nM).
CAY 10465 (Compound 4i) is a selective and high-affinity AhR receptor agonist, with a Ki of 0.2 nM, and shows no effect on estrogen receptor (Ki >100000 nM)[1]. CAY 10465 (0.01 nM-100 μM) reduces apolipoprotein A-I (apo A-I) levels in HepG2 cells, and inhibits the synthesis of the protein[2].
参考文献:
[1]. de Medina P, et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. J Med Chem. 2005 Jan 13;48(1):287-91.
[2]. Naem E, et al. Inhibition of apolipoprotein A-I gene by the aryl hydrocarbon receptor: a potential mechanism for smoking-associated hypoalphalipoproteinemia. Life Sci. 2012 Jul 26;91(1-2):64-9.
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