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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

用途

CH-223191是有效且特异性的芳烃受体(AhR) 拮抗剂。 CH-223191阻断TCDD与AhR的结合,IC50 为0.03 µM。

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名称

[ CAS 号 ]:
301326-22-7

[ 中文名 ]:
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

[ 英文名 ]:
CH-223191

[英文别名 ]:

UNII-HYE7315Z4C
AhR Antagonist
CH-223191

生物活性

[ 描述 ]:

CH-223191是有效且特异性的芳烃受体(AhR) 拮抗剂。 CH-223191阻断TCDD与AhR的结合,IC50 为0.03 µM。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[参考文献]

[1]. Zhao B, et al. CH223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor. Toxicol Sci. 2010 Oct;117(2):393-403.

[2]. Kim SH, et al. 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.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
469.4±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₉H₁₉N₅O

[ 分子量 ]:
333.387

[ 闪点 ]:
237.7±28.7 °C

[ 精确质量 ]:
333.158966

[ PSA ]:
75.13000

[ LogP ]:
3.48

[ 外观性状 ]:
orange-brown

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.633

[ 储存条件 ]:
Store at +4°C

[ 水溶解性 ]:
DMSO: ≥20mg/mL

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
22

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

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Toxicol. Appl. Pharmacol. 280(3) , 502-10, (2014)

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Analysis of Glycogen Synthase Kinase Inhibitors That Regulate Cytochrome P450 Expression in Primary Human Hepatocytes by Activation of β-Catenin, Aryl Hydrocarbon Receptor and Pregnane X Receptor Signaling.

Toxicol. Sci. 148 , 261-75, (2015)

Cytochrome P450 (CYP) expression and activity are not homogeneous in the liver lobules. Indeed, CYPs are mainly expressed and induced in centrilobular hepatocytes. The wingless-type MMTV integration s...

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