(±)-(3R*,4S*)-2-Oxo-4-phenyl-3-pyrollidinecarboxylicacid2-[1-(3-bromophenyl)ethylidene]hydrazide

Uses

AC 264613 is a selective protease-activated receptor 2 (PAR-2) agonist. AC 264613 can be used to investigate the physiological roles of the PAR-?2 receptors.

Biological Activity

ac 264613 is a potent agonist of par2 with pec50 value of 7.5 and potencies range from 30 to 100 nm [1, 2].protease-activated receptor 2 (par2) also known as coagulation factor ii (thrombin) receptor-like 1 (f2rl1) or g-protein coupled receptor 11 (gpr11) is expressed in vascular tissue and highly vascular organs and involves in the vascular tone regulation. it has been shown that par2 plays a pivotal role in vessel inflammation and wound healing processes [2].ac 264613 is a selective par2 agonist and has no effect on other pars. when tested with hek 293 t cells (par2 wild type) and knrk cells (transfected with human par2 receptors) for stimulates pi hydrolysis and ca2+ mobilization assays, ac 264613 showed effect with pec50 value of 6.9 and 7.0,respectively [1]. using quickchange mutagenesis manner, nih 3t3 cells were made with ecl2 mutations in q233e, e232r, e232r/q233r, f240s, and f240s/s37p receptors and ac 264613 treatment par2 f240s receptors were constitutively expressed in multiple functional endpoints while had no effect on e232 and q233 mutaions [2].in male sprague-dawley rat model with acute thermal nociception and edema in paw induced by sligrl-nh2 or trypsin, intrapaw administration of ac 264613 induced hind paw edema and thermal hyperalgesia at the doses as low as 30 ng and showed dose-dependent pronociceptive effects [1].

storage

Store at -20°C

References

[1]. gardell, l.r., et al., identification and characterization of novel small-molecule protease-activated receptor 2 agonists. j pharmacol exp ther, 2008. 327(3): p. 799-808.
[2]. ma, j.n. and e.s. burstein, the protease activated receptor 2 (par2) polymorphic variant f240s constitutively activates par2 receptors and potentiates responses to small-molecule par2 agonists. j pharmacol exp ther, 2013. 347(3): p. 697-704.