IF 10
PMID: 41239394 ↗CH 223191
Catalog No.: GC16220Purity:>98.00%
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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 301326-22-7
5mgIn Stock
$42.00
1
10mgIn Stock
$71.00
1
25mgIn Stock
$144.00
1
50mgIn Stock
$223.00
1
100mgIn Stock
$363.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 5mg | $42.00 | In Stock | 1 | |
| 10mg | $71.00 | In Stock | 1 | |
| 25mg | $144.00 | In Stock | 1 | |
| 50mg | $223.00 | In Stock | 1 | |
| 100mg | $363.00 | In Stock | 1 |
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Citations
2 publicationsPublications from researchers using this productDescription
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.
Protocol
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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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Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
301326-22-7
Chemical Name
2-methyl-N-[2-methyl-4-[(2-methylphenyl)diazenyl]phenyl]pyrazole-3-carboxamide
SMILES
CC1=CC=CC=C1N=NC2=CC(=C(C=C2)NC(=O)C3=CC=NN3C)C
Molecular Formula
C19H19N5O
Molecular Weight
333.39
Solubility
≥ 33.3mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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