Atopaxar

Names

[ Name ]:
Atopaxar

[Synonym ]:
Atopaxar
UNII-HTI275SD2D
E-5555

Biological Activity

[Description]:

Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar interferes with platelet signaling. Atopaxar 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 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 inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner[2]. Atopaxar 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.) prolongs the time to occlusion by 1.8-fold and 2.4-fold, respectively, compared with controls[2]. Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg[2]. Animal Model: Guinea pigs, photo-chemically-induced thrombosis (PIT) model[2] Dosage: Oral administration Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg Result: At 30 and 100 mg/kg prolonged the time to occlusion by 1.8-fold and 2.4-fold, 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 ]:
C₂₉H₃₈FN₃O₅

[ Molecular Weight ]:
527.62800

[ Exact Mass ]:
527.28000

[ PSA ]:
84.32000

[ LogP ]:
4.89230

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.