1-甲基-N-[2-METHYL-4-[2-(2-甲苯基)二氮烯基]苯基-1H
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产品名称:1-甲基-N-[2-METHYL-4-[2-(2-甲苯基)二氮烯基]苯基-1H-吡唑-5-甲酰胺CAS:301326-22-7别名：1-甲基-N-[2-METHYL-4-[2-(2-甲苯基)二氮烯基]苯基-1H-吡唑-5-甲酰胺;1-甲基-N-[2-甲基-4-[(2-甲基苯基)偶氮]苯基]-1H-吡唑-5-甲酰胺英文名：1-Methyl-N-[2-methyl-4-[2-(2-methylphenyl)diazenyl]phenyl-1H-pyrazole-5-carboxamide
- 生物活性CH-223191是一种有效的特定aryl hydrocarbon receptor (AhR)拮抗剂，IC50为30 nM。
- 体外研究CH-223191 blocks TCDD-mediated nuclear translocation and DNA binding of AhR, and also causes the inhibition of TCDD-induced cytochrome P450 enzyme activity. In human glioblastoma cells, CH-223191downregulates the TGF-beta/Smad pathway, and reduces clonogenic survival and invasiveness. In SK-N-SH human-derived neuronal cells, CH223191 counteracts the TCDD-induced suppression of neuronal acetylcholinesterase expression. In endothelial cells, CH-223191 potentiates ICAM-1 expression and prevents RelB nuclear translocation.
- 体内研究CH-223191 (10 mg/kg/day, p.o.) potently prevents TCDD-caused cytochrome P450 induction, liver toxicity, and wasting syndrome in mice.
