A potent, and selective PAR2 antagonist with Kd of 13.5 nM.
CAS：2100284-59-9
分子式：C30H27BrN4O3
分子量：571.46
纯度：98%
存储：Store at -20°C

Background:

AZ3451 is a protease-activated receptor-2 (PAR2) antagonist.

AZ3451 is highly lipophilic, which coincides with the hydrophobic nature of the binding pocket within the membrane. The interaction of AZ3451 with PAR2 is predominately hydrophobic in nature. AZ3451 binds to a remote allosteric site outside the helical bundle, which prevents structural rearrangements required for receptor activation and signaling.

IC₅₀/K_D

IP-One(SLIGRL)	23±1nM(n=72)
FLIPR(SLIGRL)	5.4±1.1nM(n=11)
FLIPR(Trypsin)	6.6±1.1μM(n=9)
Biacore(KD)	13.5±3nM(n=3)
β-arrestin-2(PAR1)	>50μM(n=1)
β-arrestin-2(PAR2)	<2.5nM(n=1)
β-arrestin-2(PAR4)	0.38μM(n=1)

参考文献:
1. Cheng RKY, et al. Structural insight into allosteric modulation of protease-activated receptor 2. Nature. 2017 May 4;545(7652):112-115.