PAR2 antagonist C781

Chemical Structure : PAR2 antagonist C781

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货号: PC-20882Not For Human Use, Lab Use Only.

PAR2 antagonist C781 is a potent β-Arrestin biased protease-activated receptor-2 (PAR2) antagonist, effectively reduces 2AT, trypsin and elastase-induced signalling in vitro physiological assays.

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生物&药学活性

PAR2 antagonist C781 is a potent β-Arrestin biased protease-activated receptor-2 (PAR2) antagonist, effectively reduces 2AT, trypsin and elastase-induced signalling in vitro physiological assays.
C781 antagonizes PAR2 signalling following peptidomimetic and proteinase-mediated receptor activation in cells naturally expressing the human PAR2 receptor.
C781 effectively reduces 2AT-induced (600 nM) MAPK phosphorylation in a concentration-dependent fashion with significant inhibitory effects using signalling-specific assays in 16HBE14o- cells, with no effect on the Gq/Ca2+ signalling pathway.
C781 reduces airway hyperresponsiveness, limits acute A. alternata-induced inflammation in an acute A. alternata exposure model.
C781 limits acute A. alternata-induced production of inflammatory cytokines, shows limited effect on acute A. alternata-induced airway epithelial mucin expression.

物理化学性质&存储条件

分子量	515.66
分子式	C27H41N5O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	CC(C)CC(N[C@H]1CN(C(C2=CC=CO2)=O)C(CN(CC3CCNCC3)C([C@@H]4CC(C)C)=O)N4C1=O)=O

参考文献

1. Hillary V Schiff, et al. Br J Pharmacol. 2023 Mar;180(5):667-680.