Potent and selective protease-activated receptor 2 (PAR2
) agonist (pEC50
= 7.5). Displays no activity at other PAR subtypes and exhibits no significant activity at over 30 other receptors implicated in nociception and inflammation. Stimulates PI hydrolysis, Ca2+
mobilization and cellular proliferation in vitro
values are 6.9, 7.0 and 7.5 respectively).
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All Tocris products are intended for laboratory research use only.
Discovery of potent and selective small-molecule PAR-2 agonists.
Seitzberg et al.
Identification and characterization of novel small-molecule protease-activated receptor 2 agonists.
Gardell et al.