CH-223191

CH-223191 is a potent, specific antagonist of AhR (aryl hydrocarbon receptor), potently inhibits TCDD-induced AhR-dependent transcription with IC50 of 0.03 uM; shows more inhibitory potency and no agonist-like effect, compared with flavone, resveratrol, and α-naphthoflavone, as well as estrogenic potency; inhibits TCDD-AhR binding and TCDD-induced nuclear translocation and DNA binding of AhR, prevents the expression of cytochrome P450 enzymes, target genes of the AhR; potently prevents TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. (In Vitro) :CH-223191 (0.1-10 μM; pre-treated 1 hour) inhibits TCDD-caused cytochrome P450 1A1 mRNA expression in a in dose-dependent manner.CH-223191 (0.1-10 μM; pre-treated 1 hour) causes a concentration-dependent inhibition of TCDD-induced cytochrome P450 enzyme activity. (In Vivo) :CH-223191 (10 mg/kg; once a day; 25 days) suppresses cytochrome P450 1A1 expression and the intrahepatocyte fat content in liver, reduces activity of AST and ALT in TCDD-treated mice.