CH-223191

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CH-223191  纯度: 98.71%

CH-223191 是芳烃受体 (AhR) 的有效特异性拮抗剂。 CH-223191 抑制 TCDD 介导的核转位和 AhR 的 DNA 结合。CH-223191 抑制 TCDD 诱导的荧光素酶活性的 IC50 值为 0.03 μM。

CH-223191

CH-223191 Chemical Structure

CAS No. : 301326-22-7

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CH-223191 相关产品

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生物活性

CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM[1].

体外研究
(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[1].
CH-223191 (0.1-10 μM; pre-treated 1 hour) causes a concentration-dependent inhibition of TCDD-induced cytochrome P450 enzyme activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

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[1]

Cell Line: HepG2 cells
Concentration: 0.1-10 μM
Incubation Time: 1 hour
Result: Decreased TCDD-caused cytochrome P450 1A1 protein Treatment.

体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (6 weeks old)[1]
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.

分子量

333.39

Formula

C19H19N5O
CAS 号

301326-22-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (374.94 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9995 mL 14.9974 mL 29.9949 mL
5 mM 0.5999 mL 2.9995 mL 5.9990 mL
10 mM 0.2999 mL 1.4997 mL 2.9995 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.50 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. 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. Epub 2006 Mar 15.