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2-methyl-2H-pyrazole-3-carboxylic acid; AhR Antagonist
CH-223191 is a synthetic antagonist for the cytosolic aryl hydrocarborn receptor (AhR) transcription factor .
It exerts a ligand-selective antagonism and appears to be more effective on halogenated aromatic hydrocarbons such as the xenobiotic 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), than on polycyclic aromatic hydrocarbons and non halogenated aromatic hydrocarbons such as FICZ and ITE, respectively .
Read our review on AhR's key role in the intestinal microbiota and immunity.
1. Kim, S.H. et al., 2006. 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. 69:1871-78.
2. Zhao B. et al., 2010. CH223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor. Toxicol. Sci. 117:393-403.
Inhibition of AhR activity by CH-223191 in HepG2-Lucia™ Ahr cells.
The cells were stimulated with 30 nM TCDD or 30 μM ITE in the presence of 10 μM CH-223191. After overnight incubation, the AhR response was assessed by determining Lucia luciferase activity in the supernatant using.QUANTI-Luc™.
Percentages of the maximal response for the ligand with no inhibitor are shown.
CAS number: 301326-22-7
Synonym: 2-methyl-2H-pyrazole-3-carboxylic acid
Solubility: 90 mM (30 mg/ml) in DMSO
Working concentration: 1µM (333 ng/ml) to 30 µM (10.1 μg/ml) for cell culture assays
Molecular weight: 333.4 g/mol
- Purity ≥ 95% (UHPLC).
- The absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ TLR2 and HEK‑Blue™ TLR4 cells.
- The inhibitory activity has been validated using cellular assays.
10 mg CH-223191
CH-223191 is shipped at room temperature.
Store at -20°C.
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