Bioactivity | AC-55541 is a highly selective protease-activated receptor 2 (PAR2) agonist (pEC50=6.7), displays no activity at other PAR subtypes or at over 30 other receptors involved in nociception and inflammation. AC-55541 has pEC50 values of 5.9 and 6.6 in PI hydrolysis assays and Ca2+ mobilization assays and exhibits pronociceptive activity in vivo[1]. | ||||||||||||
Target | pEC50: 6.7 (PAR2) | ||||||||||||
Invitro | AC-55541 (100 nM; 1 hour) suppresses poly I:C–induced CXCL10 mRNA in NHBE cells[2]. RT-PCR[2] Cell Line: | ||||||||||||
Name | AC-55541 | ||||||||||||
CAS | 916170-19-9 | ||||||||||||
Formula | C25H20BrN5O3 | ||||||||||||
Molar Mass | 518.36 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Gardell LR, et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808. [2]. Homma T, et al. Role of Aspergillus fumigatus in Triggering Protease-Activated Receptor-2 in Airway Epithelial Cellsand Skewing the Cells toward a T-helper 2 Bias. Am J Respir Cell Mol Biol. 2016 Jan;54(1):60-70. |