For research use only. Not for therapeutic Use.
Potent and orally active thrombin receptor (or protease-activated receptor 1, PAR1) antagonist (IC50: 19 nM); E5555 showed potent inhibitory effects on human platelet aggregation induced by thrombin and TRAP with IC50 values of 64 and 31nM, respectively
| Catalog Number | I022620 |
| CAS Number | 474550-69-1 |
| Molecular Formula | C29H38FN3O5.HBr |
| Purity | ≥95% |
| IUPAC Name | 1-(3-tert-butyl-4-methoxy-5-morpholin-4-ylphenyl)-2-(5,6-diethoxy-4-fluoro-3-imino-1H-isoindol-2-yl)ethanone;hydrobromide |
| InChI | InChI=1S/C29H38FN3O5.BrH/c1-7-37-23-15-19-16-33(28(31)24(19)25(30)27(23)38-8-2)17-22(34)18-13-20(29(3,4)5)26(35-6)21(14-18)32-9-11-36-12-10-32;/h13-15,31H,7-12,16-17H2,1-6H3;1H |
| SMILES | CCOC1=C(C(=C2C(=C1)CN(C2=N)CC(=O)C3=CC(=C(C(=C3)N4CCOCC4)OC)C(C)(C)C)F)OCC.Br |
| Reference | LV Serebruany et al. The in-vitro effects of E5555, a protease-activated receptor (PAR)-1 antagonist, on platelet biomarkers in healthy volunteers and patients with coronary artery disease. Thromb. Haemost. 2009, 102(1), 111-119.
S Goto et al. Double-blind, placebo-controlled Phase II studies of the protease-activated receptor 1 antagonist E5555 (atopaxar) in Japanese patients with acute coronary syndrome or high-risk coronary (…). Eur. Heart J. 2010, 31(21), 2601-2613.
M Kogushi et al. The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs. Eur. J. Pharmacol. 2011, 657(1-3), 131-137.
Y Kai et al. Prevention of the hypercontractile response to thrombin by proteinase-activated receptor-1 antagonist in subarachnoid hemorrhage. Stroke. 2007 Dec;38(12):3259-65. |
