(S)-2-(6-bromobenzo[d][1,3]dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1H-benzo[d]imidazole-5-carboxamide

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

(S)-2-(6-bromobenzo[d][1,3]dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1H-benzo[d]imidazole-5-carboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden

• Verwenden

  AZ3451 has been used as a protease-activated receptor 2 (PAR-2) antagonist to study the involvement of PAR-2 receptors in factor X activated (FXa)-induced upregulation of the cell adhesion molecules.

• Definition

  ChEBI: AZ3451 is a member of the class of benzimidazoles that is 1H-benzimidazole substituted by (1S)-1-cyclohexylethyl, 6-bromo-1,3-benzodioxol-5-yl, and 4-(cyanoanilino)acyl groups at positions 1, 2 and 5, respectively. It is an allosteric modulator of protease-activated receptor 2 (IC50 = 23 nM) and exhibits anti-osteoarthritis properties. It has a role as an anti-inflammatory agent, a PAR2 negative allosteric modulator and an autophagy inducer. It is a secondary carboxamide, a nitrile, a member of benzimidazoles, a member of benzodioxoles and an organobromine compound.

• Biologische Aktivität

  AZ3451 is a potent protease-activated receptor 2 (PAR2) antagonist that binds to a distant allosteric site outside the helical bundle with an IC50 of 23 nM.

• in vitro

  Antagonist AZ3451 binds to a remote allosteric site outside the helical bundle of the protease-activated receptor 2. AZ3451 is highly lipophilic, which coincides with the hydrophobic nature of the binding pocket within the membrane. Antagonist binding prevents structural rearrangements required for receptor activation and signalling.

• target

  Target	Value
  PAR2 (Cell-free assay)	23 nM

(S)-2-(6-bromobenzo[d][1,3]dioxol-5-yl)-N-(4-cyanophenyl)-1-(1-cyclohexylethyl)-1H-benzo[d]imidazole-5-carboxamide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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