182705

AhR Antagonist

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

• Synonyme(s) : 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
• Formule empirique (notation de Hill): C₁₉H₁₉N₅O
• Numéro CAS: 301326-22-7
• Poids moléculaire : 333.39
• Numéro MDL: MFCD00377884
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: orange-brown
• Solubilité: DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°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+
• Clé InChI: LKTNEXPODAWWFM-GHVJWSGMSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable