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CH-223191

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Chemical Structure| 301326-22-7 同义名 : -
CAS号 : 301326-22-7
货号 : A525118
分子式 : C19H19N5O
纯度 : 99%+
分子量 : 333.387
MDL号 : MFCD00377884
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(314.95 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AhR

    AhR, IC50:30 nM
描述 The aryl hydrocarbon (dioxin) receptor (AhR) is a ligand-dependent basic helix-loop-helix-Per-Arnt-Sim (PAS)–containing transcription factor that responds to exogenous and endogenous chemicals with the induction/repression of expression of a diverse battery of genes in a wide range of species and tissues. CH-223191 is a preferential inhibitor of TCDD-induced AhR-dependent gene expression in various species. The relative inhibitory potency (IC50) of CH-223191 against TCDD-dependent gene induction in each cell line was 1.1 μM for guinea pig cells, 1.5 μM for mouse cells, 3.1 μM for rat cells, and 0.2 μM for human cells. Co-incubation of yAHAYc6 cells with CH-223191 dramatically reduced TCDD-dependent nuclear accumulation of yAhR (yellow fluorescent protein (YFP)-AhR chimera). The ability of 10 μM CH-223191 to significantly inhibit induction by the dihalogen-substituted flavonoid AY9 in rat hepatoma cells indicates this concentration of CH-223191 appears to have a preference for halogen-substituted AhR agonists [1]. It is noteworthy that CH-223191 potently prevented TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice [2].
作用机制 CH223191 could bind to the AhR outside of the ligand–binding domain and act as an allosteric modulator.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.00mL

0.60mL

0.30mL

15.00mL

3.00mL

1.50mL

30.00mL

6.00mL

3.00mL
参考文献

[1]Zhao B, Degroot DE, Hayashi A, He G, Denison MS. CH223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor. Toxicol Sci. 2010 Oct;117(2):393-403. doi: 10.1093/toxsci/kfq217. Epub 2010 Jul 15. PMID: 20634293; PMCID: PMC2940411.

[2]Kim SH, Henry EC, Kim DK, Kim YH, Shin KJ, Han MS, Lee TG, Kang JK, Gasiewicz TA, Ryu SH, Suh PG. Novel compound 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) prevents 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor. Mol Pharmacol. 2006 Jun;69(6):1871-8. doi: 10.1124/mol.105.021832. Epub 2006 Mar 15. PMID: 16540597.