CH 223191 |
| カタログ番号GC16220 |
CH 223191 は、アリール炭化水素受容体 (AhR) の強力かつ特異的なアンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 301326-22-7
Sample solution is provided at 25 µL, 10mM.
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.
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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 | |
| Chemical Name | 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 | ||
| Formula | C19H19N5O | M.Wt | 333.39 |
| 溶解度 | ≥ 33.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9995 mL | 14.9975 mL | 29.9949 mL |
| 5 mM | 0.5999 mL | 2.9995 mL | 5.999 mL |
| 10 mM | 0.2999 mL | 1.4997 mL | 2.9995 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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