产品描述:
I-191 is an antagonist of proteinase-activated receptor 2 (PAR2; IC50 = 72.4 nM in HT-29 cells expressing the human receptor).{68527} It inhibits trypsin-induced calcium release in HT-29 cells (IC50 = 200 nM for the human receptor). I-191 (0.1, 1, and 10 µM) reduces the migration of HT-29 cells in a scratch assay. It decreases the expression of mRNA encoding chemokine (C-X-C motif) ligand 8 (CXCL8) in, and secreted IL-8 levels from, HT-29 cells induced by the PAR2 agonist 2f-LIGRL-NH2 when used at a concentration of 1 and 10 µM. Ex vivo, I-191 (10 µM) inhibits tissue factor-induced clotting using isolated human whole blood.{68528}