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Chemical Structure : PAR2 antagonist C781
Catalog No.: 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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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.
| M.Wt | 515.66 | |
| Formula | C27H41N5O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Hillary V Schiff, et al. Br J Pharmacol. 2023 Mar;180(5):667-680.
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