AC-264613

SKU: orb1223443

Description

AC-264613 is the first agonist of the G-protein-coupled receptor (GPCR) protease activated receptor 2 (PAR2). AC-264613 suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages. AC-264613 activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 30 to 100 nM.

Key Properties

• CAS Number: 1051487-82-1
• MW: 400.28
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₈BrN₃O₂
• SMILES: O=C([C@H]1C(=O)NC[C@@H]1c1ccccc1)N/N=C(/c1cccc(Br)c1)\C
• Target: PAR-2

Bioactivity

• In Vivo:
  AC-264613 exhibits moderate elimination half-live (T1/2 = 2.5±2.0 h) following i.p. administration (10 mg/kg) in male Sprague-Dawley rats.
• In Vitro:
  AC-264613 (10 μM; for 6 hours) causes a decrease of IRF5 expression and also significantly reduces p53 protein expression in macrophages. Western blot analysis. Cell line: Granulocyte-macrophage colony-stimulating factor (GM-CSF)-dependent macrophages. Concentration: 10 μM. Incubation time: 6 hours. Result: Significantly decreased IRF5 expression and reduced p53 protein levels.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AC-264613 | AC 264613 | AC264613

Quick Database Links

Gene Symbol

PAR-2