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Atopaxar hydrobromide

Names

[ CAS No. ]:
474550-69-1

[ Name ]:
Atopaxar hydrobromide

[Synonym ]:
K3D2WJ7U0I
2-(5,6-Diethoxy-7-fluoro-1-imino-1,3-dihydro-2H-isoindol-2-yl)-1-[4-methoxy-3-(2-methyl-2-propanyl)-5-(4-morpholinyl)phenyl]ethanone hydrobromide (1:1)
E 5555 hydrobromide
Ethanone, 2-(5,6-diethoxy-7-fluoro-1,3-dihydro-1-imino-2H-isoindol-2-yl)-1-[3-(1,1-dimethylethyl)-4-methoxy-5-(4-morpholinyl)phenyl]-, hydrobromide (1:1)
Atopaxar hydrobromide
MFCD25371545

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> Protease-Activated Receptor (PAR)

[Target]

PAR-1[1]


[In Vitro]

Atopaxar hydrobromide (0.0001-10 μM; 1h) inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC50 of 0.019 μM[2]. Atopaxar hydrobromide inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner[2]. Atopaxar hydrobromide does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM[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.

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H39BrFN3O5

[ Molecular Weight ]:
608.539

[ Exact Mass ]:
607.205688

[ Storage condition ]:
-20°C

Related Compounds