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E 5555 hydrobromide
- Atopaxar hydrobromide
Axon 2030
- Parent CAS: 751475-53-3
Purity:
99%
- Soluble in DMSO
- MF: C29H38FN3O5.HBr
- MW: 608.54
Description
E 5555 hydrobromide (Atopaxar) is a potent, orally active protease-activated receptor 1 (PAR1/thrombin receptor) antagonist with reported IC50 activity of 19 nM. It inhibits thrombin- and TRAP-induced human platelet aggregation in reported assays.
PAR1 mediates thrombin-dependent platelet activation and vascular inflammatory signaling. E 5555 is pharmacologically relevant for studying antiplatelet mechanisms, thrombin receptor blockade and cardiovascular thrombosis research.
Key Features
- Potent PAR1 antagonist
- Reported IC50: 19 nM
- Inhibits thrombin- and TRAP-induced platelet aggregation
- Orally active antiplatelet pharmacology
Applications
- PAR1 receptor assays
- Platelet aggregation studies
- Thrombin signaling research
- Antithrombotic pharmacology models
More Information
| Parent CAS No. | 751475-53-3 |
|---|---|
| Chemical Name | 1-(3-tert-butyl-4-methoxy-5-morpholinophenyl)-2-(5,6-diethoxy-7-fluoro-1-iminoisoindolin-2-yl)ethanone hydrobromide |
| SMILES | C(=O)(C1=CC(N2CCOCC2)=C(OC)C(C(C)(C)C)=C1)CN1CC2=C(C1=N)C(F)=C(OCC)C(OCC)=C2.Br |
| MFCD | N.A. |
| 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 |
| InChiKey | UNMBLVOFOAGGCG-UHFFFAOYSA-N |
| CID | 22929978 |
| Short Description | PAR1 antagonist |
E 5555 hydrobromide (Atopaxar)
potent PAR1 antagonist
E 5555 hydrobromide
Atopaxar
Atopaxar hydrobromide
E5555
E-5555
PAR1
Antagonist
PAR1 receptor assays
Platelet aggregation studies
Thrombin signaling research
Antithrombotic pharmacology models
inflammation
cardiovascular research
vascular biology
thrombosis
signal transduction
receptor pharmacology
CAS 751475-53-3
CAS 474550-69-1
Axon Medchem
Axon 2030
Supplier
Vendor
References
- 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.
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