182705
AhR Antagonist
2-Methyl-2H-pyrazole-3-carboxylic acid-(2-methyl-4-o-tolyl-azophenyl)-amide, CH-223191
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
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Fax: +49 6151 72 2000
31 May 2012
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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 |
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