CH-223191

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CH-223191 是一种有效的、特异性的 AhR（芳烃受体）拮抗剂，有效抑制 TCDD 诱导的 AhR 依赖性转录，IC50 为 0.03 uM。

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.

CH-223191 (0.1-10 μM; pre-treated 1 hour)inhibits TCDD-causedcytochrome 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.RT-PCR Cell Line:HepG2 cells Concentration:0.1-10 μM Incubation Time:1 hour Result:Caused inhibition of TCDD-induced cytochrome P450 mRNA expression.Western Blot Analysis Cell Line:HepG2 cells Concentration:0.1-10 μM Incubation Time:1 hour Result:Decreased TCDD-caused cytochrome P450 1A1 protein Treatment.

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. Animal Model:Male ICR mice (6 weeks old)Dosage:10 mg/kg Administration:10 mg/kg; once a day; 25 days Result:Prevented TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice.

CH223191

Endocrinology/Hormones

AhR

AhR

Inflammation/Immunology

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301326-22-7

333.3871

C19H19N5O

>98% (HPLC)

DMSO: ≥ 35 mg/mL

O=C(C1=CC=NN1C)NC2=CC=C(/N=N/C3=CC=CC=C3C)C=C2C

1H-Pyrazole-5-carboxamide, 1-methyl-N-[2-methyl-4-[2-(2-methylphenyl)diazenyl]phenyl]-

(-20℃)

With Ice Pack

≥ 2 years