| Identification | Back Directory | [Name]
Atopaxar hydrobromide | [CAS]
474550-69-1 | [Synonyms]
ER 172594-06
ER 172594-06 HBr
E 5555 hydrobromide
Atopaxar hydrobromide
ATOPAXAR HYDROBROMIDE; ER-172594-06; E5555 | [Molecular Formula]
C29H39BrFN3O5 | [MDL Number]
MFCD25371545 | [MOL File]
474550-69-1.mol | [Molecular Weight]
608.539 |
| Hazard Information | Back Directory | [Uses]
Atopaxar (E5555) hydrobromide is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar hydrobromide, an antiplatelet agent, interferes with platelet signaling. Atopaxar hydrobromide can be used for the research of atherothrombotic disease[1][2]. | [in vivo]
Atopaxar (30-100 mg/kg; p.o.) hydrobromide causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model[2].
Atopaxar hydrobromide does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2].
| Animal Model: | Guinea pigs, PIT model[2] | | Dosage: | Oral administration | | Administration: | 10 mg/kg, 30 mg/kg, 100 mg/kg
| | Result: | Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls. |
| [IC 50]
PAR1: 5.1 nM (IC50) | [References]
[1] Chris Dockendorff, et al. Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett. 2012 Mar 8; 3(3): 232–237. DOI:10.1021/ml2002696
[2] Motoji 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 Apr 25;657(1-3):131-7. DOI:10.1016/j.ejphar.2011.01.058
[3] Sun J, et al., Discovery and evaluation of Atopaxar hydrobromide, a novel JAK1 and JAK2 inhibitor, selectively induces apoptosis of cancer cells with constitutively activated STAT3. Invest New Drugs. 2020 Aug;38(4):1003-1011. DOI:10.1007/s10637-019-00853-w |
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