AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist which displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. It activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM. It was well absorbed when administered intraperitoneally to rats, reaching micromolar peak plasma concentrations. It was stable to metabolism by liver microsomes and maintained sustained exposure in rats.
Products > Drug Discovery > Inhibitor | Products > Drug Discovery > Inhibitor | Cardiovascular and blood system | Protease-Activated Receptors (PARs)
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