182705

AhR Antagonist

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

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₉H₁₉N₅O
• Numer CAS: 301326-22-7
• Masa cząsteczkowa: 333.39
• Numer MDL: MFCD00377884
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: orange-brown
• rozpuszczalność: DMSO: 10 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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+
• Klucz InChI: LKTNEXPODAWWFM-GHVJWSGMSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Irritant (B)

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable