FSLLRY-NH2 TFA (FSY-NH2) is a selective protease-activated receptor 2 (PAR2) inhibitor with an ic50 of 50 ?M in PAR2-KNRK cells.
FSLLRY-NH2 blocks the ability of trypsin to activate PAR(2) either in PAR(2)-expressing Kirsten virus-transformed kidney (KNRK) cell lines or in a rat aorta ring preparation. The mechanism of this activity does not involve a simple inhibition of trypsin proteolytic activity, but possibly by interacting with a tethered ligand receptor-docking site.[1]
Treatment with FSLLRY-NH2 significantly improves neurological outcome and reduces the number of degenerating hippocampal neurons after ACA (asphyxial CA).[2]
[1] Bahjat Al-Ani , et al. J Pharmacol Exp Ther. 2002 Feb;300(2):702-8. [2] Umut Ocak, et al. Turk Neurosurg. 2020;30(2):244-251.