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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。

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

The aryl hydrocarbon receptor suppresses osteoblast proliferation and differentiation through the activation of the ERK signaling pathway.

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

Ahr activation is known to be associated with synovitis and exacerbated rheumatoid arthritis (RA), but its contributions to bone loss have not been completely elucidated. Osteoblast proliferation and ...

In-vitro evidence of enhanced breast cancer resistance protein-mediated intestinal urate secretion by uremic toxins in Caco-2 cells.

J. Pharm. Pharmacol. 67(2) , 170-7, (2015)

It has been reported that intestinal urate excretion is increased at chronic kidney disease (CKD) state. In this report, whether uremic toxins are involved in the upregulation of intestinal breast can...

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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