I-191

I-191 is an antagonist of proteinase-activated receptor 2 (PAR2, IC50 = 72.4 nM in HT-29 cells expressing the human receptor). 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.Formal Name: 4-[[8-(1,1-dimethylethyl)-6-(4-fluorophenyl)imidazo[1,2-b]pyridazin-2-yl]carbonyl]-3,3-dimethyl-2-piperazinone. CAS Number: 1690172-25-8. Molecular Formula: C23H26FN5O2. Formula Weight: 423.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Methanol: Soluble. lambdamax: 245, 283 nm. SMILES: O=C(N1CCNC(C1(C)C)=O)C2=CN3N=C(C4=CC=C(F)C=C4)C=C(C(C)(C)C)C3=N2. InChi Code: InChI=1S/C23H26FN5O2/c1-22(2,3)16-12-17(14-6-8-15(24)9-7-14)27-29-13-18(26-19(16)29)20(30)28-11-10-25-21(31)23(28,4)5/h6-9,12-13H,10-11H2,1-5H3,(H,25,31). InChi Key: DTASTQAQBOZSRR-UHFFFAOYSA-N.