AC 264613

Names

[ Name ]:
AC 264613

[Synonym ]:
UNII-1ST2P4BE17
3-Pyrrolidinecarboxylic acid,2-oxo-4-phenyl-,2-(1-(3-bromophenyl)ethylidene)hydrazide,(3R,4S)-rel
AC 264613

Biological Activity

[Description]:

AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Protease-Activated Receptor (PAR)

Research Areas >> Inflammation/Immunology

[Target]

pEC50: 7.5 (PAR-2)[1]

[In Vitro]

AC-264613 (10 μM; for 6 hours) causes a decrease of IRF5 expression and also significantly reduces p53 protein expression in macrophages[2]. Western Blot Analysis[2] 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.

[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[3].

[References]

[1]. Jimmi Gerner Seitzberg, et al. Discovery of potent and selective small-molecule PAR-2 agonists. J Med Chem. 2008 Sep 25;51(18):5490-3.

[2]. Rui Yamaguchi, et al. A protease-activated receptor 2 agonist (AC-264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages: Role of p53. Cell Biol Int. 2016 Jun;40(6):629-41.

[3]. Luis R Gardell, et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808.