AhR Antagonist-CAS 301326-22-7-Calbiochem

C₁₉H₁₉N₅O

333.39

MFCD00377884

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.

Cell permeable: yes
Target IC₅₀: 30 nM in blocking TCDD-induced AhR transcription activity in HepG2 cells in vitro
Product does not compete with ATP.
Reversible: no
Primary Target
AhR (aryl hydrocarbon receptor)

Toxicity: Irritant (B)

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

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

100

≥95% (HPLC)

Calbiochem^®

OK to freeze
protect from light

orange-brown

DMSO: 10 mg/mL

ambient

2-8℃

10 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3