182705

CH-223191

The AhR Antagonist, also referenced under CAS 301326-22-7, controls the biological activity of AhR.

• Synonyma: AhR Antagonist, 2-Methyl-2H-pyrazole-3-carboxylic acid-(2-methyl-4- o-tolyl-azophenyl)-amide, CH-223191, 2-Methyl-2H-pyrazole-3-carboxylic acid-(2-methyl-4-o-tolyl-azophenyl)-amide, CH-223191
• Empirický vzorec (Hillův zápis): C₁₉H₁₉N₅O
• Číslo CAS: 301326-22-7
• Molekulová hmotnost: 333.39
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00377884
• Assay: ≥95% (HPLC)
• Form: (Orange-brown)
• Storage condition: OK to freeze, protect from light

Vlastnosti

• Název produktu: AhR Antagonist, The AhR Antagonist, also referenced under CAS 301326-22-7, controls the biological activity of AhR.
• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: (Orange-brown)
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: orange-brown
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [n]1(nccc1C(=O)Nc2c(cc(cc2)\N=N\c3c(cccc3)C)C)C
• InChI: 1S/C19H19N5O/c1-13-6-4-5-7-17(13)23-22-15-8-9-16(14(2)12-15)21-19(25)18-10-11-20-24(18)3/h4-12H,1-3H3,(H,21,25)/b23-22+
• InChI key: LKTNEXPODAWWFM-GHVJWSGMSA-N

Popis

General description

A cell-permeable pyrazolo-amide compound that potently blocks the binding of TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) to AhR (aryl hydrocarbon receptor) in a dose-dependent manner. Shown to Inhibit TCDD-induced AhR transcription activity in HepG2 cells in vitro (IC₅₀ = 30 nM) and prevent TCDD-elicited liver toxicity and wasting syndrome in mice in vivo. Unlike the commonly used AhR antagonist flavone, this inhibitor has no effect on estrogen receptor transcription activity, nor does it exhibit TCDD-like agonist activity even at concentrations as high as 10 µM.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
AhR (aryl hydrocarbon receptor)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 30 nM in blocking TCDD-induced AhR transcription activity in HepG2 cells in vitro

Packaging

Packaged under inert gas

Other Notes

Kim, S.H., et al. 2006. Mol. Pharmacol.69, 1871.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Irritant (B)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• Co se děje?: WGK 3
• Bod vzplanutí (°F): Not applicable
• Bod vzplanutí (°C): Not applicable