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182705  AhR Antagonist

2-Methyl-2H-pyrazole-3-carboxylic acid-(2-methyl-4-o-tolyl-azophenyl)-amide, CH-223191

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25 May 2012

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182705-10MG  10 mg 
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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.
Product information
Form Orange-brown
Molar mass 333.4
Protect from Light Yes
Packaged under inert gas Yes
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C19H19N5O
CAS number 301326-22-7
Store and ship information
Storage +2°C to +8°C
Ship Ambient Temperature Only
Irritant
AhR Antagonist, molecular structure

© Merck KGaA, Darmstadt, Germany, 2012

All references to Merck refer to Merck KGaA, Darmstadt, Germany.


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