CH 223191是一种有效且特异性的芳烃受体（AhR）拮抗剂，可抑制TCDD介导的AhR核转位和DNA结合，并抑制TCDD诱导的荧光素酶活性，IC50为0.03 μM。
Cas No.:301326-22-7
Sample solution is provided at 25 µL, 10mM.
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CH 223191 is an effective and specific antagonist of the aryl hydrocarbon receptor (AhR), capable of inhibiting TCDD-mediated AhR nuclear translocation and DNA binding, and suppresses TCDD-induced luciferase activity, with an IC50 of 0.03 μM[1]. CH-223191 effectively prevents TCDD-induced cytochrome P450 induction, hepatotoxicity, and wasting syndrome in mice.
In vitro, CH 223191 (0.1-10 μM; pre-treated for 1 hour) inhibits TCDD-induced cytochrome P450 1A1 mRNA expression in a dose-dependent manner[1]. CH 223191 reduces the invasiveness of the LNT-229 cell line by 81% and the LN-308 cell line by 72%[2]. Pre-treatment with CH 223191 (10–6 M) significantly reverses the inhibition effect of TCDD (10–9 M) on human AChE promoter activity[3].
In vivo, CH 223191 (10 mg/kg; once daily; for 25 days) inhibits the expression of cytochrome P450 1A1 in the liver of mice treated with TCDD and reduces hepatic fat content, lowering AST and ALT activity[1].
References:
[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.
[2] Gramatzki D , Pantazis G , Schittenhelm J ,et al. Aryl hydrocarbon receptor inhibition downregulates the TGF-beta/Smad pathway in human glioblastoma cells[J]. Oncogene. 2009(28).
[3] Xie, Heidi Qunhui,Xu, Hai-Ming,Fu, Hua-Ling,et al. AhR-Mediated Effects of Dioxin on Neuronal Acetylcholinesterase Expression in Vitro[J].Environmental Health Perspectives, 2013, 121.
CH 223191是一种有效且特异性的芳烃受体（AhR）拮抗剂，可抑制TCDD介导的AhR核转位和DNA结合，并抑制TCDD诱导的荧光素酶活性，IC50为0.03 μM[1]。CH-223191可有效预防TCDD诱导的细胞色素P450诱导、肝毒性和小鼠消瘦综合征。
在体外，CH 223191（0.1-10 μM;预处理1小时）以剂量依赖性方式抑制TCDD诱导的细胞色素P450 1A1 mRNA表达[1]。CH 223191使LNT-229细胞系的侵袭性降低81%，使LN-308细胞系的侵袭性降低72%[2]。CH 223191（10–6 M）预处理显著逆转了TCDD（10–9 M）对人AChE启动子活性的抑制作用[3]。
在体内，CH 223191（10 mg/kg;每日一次; 25天）可抑制TCDD给药小鼠肝脏中细胞色素P450 1A1的表达和肝细胞内脂肪含量，降低AST和ALT活性[1]。
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Cell experiment [1]: |
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Cell lines |
HepG2 cell lines |
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Preparation method |
The cells were treated with different concentrations of CH223191 for 5 h. |
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Reaction Conditions |
0.1-10 μM; 5 h |
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Applications |
CH223191 was able to inhibit the catalytic activity of CYP1A1 with IC50 of 1.48 μM. CYP1A1 transcription activity caused by the CH223191 up to 16.84%. |
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Animal experiment [2]: |
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Animal models |
Male ICR mice |
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Preparation method |
Male ICR mice (6 weeks old) were given oral vehicle (corn oil) or CH-223191 (10 mg/kg in corn oil) once a day for 25 days and treated i.p. with TCDD (100g/kg in corn oil) once after the first week of CH-223191 treatment. The body weights of all mice were measured before dosing and at termination. |
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Dosage form |
10 mg/kg; 25 days ; oral |
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Applications |
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. |
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References: [1] Mohammadi-Bardbori A , Omidi M , Arabnezhad M R. Impact of CH223191-Induced Mitochondrial Dysfunction on Its Aryl Hydrocarbon Receptor Agonistic and Antagonistic Activities[J]. Chemical Research in Toxicology, 2019. [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. |
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| Cas No. | 301326-22-7 | SDF | |
| 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 | ||
| 化学名 | 2-methyl-N-[2-methyl-4-[(2-methylphenyl)diazenyl]phenyl]pyrazole-3-carboxamide | ||
| Canonical SMILES | CC1=CC=CC=C1N=NC2=CC(=C(C=C2)NC(=O)C3=CC=NN3C)C | ||
| 分子式 | C19H19N5O | 分子量 | 333.39 |
| 溶解度 | ≥ 33.3mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9995 mL | 14.9975 mL | 29.9949 mL |
| 5 mM | 599.9 μL | 2.9995 mL | 5.999 mL |
| 10 mM | 299.9 μL | 1.4997 mL | 2.9995 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet