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Atopaxar

Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease[1][2].

Product Specifications

CAS Number

[751475-53-3]

Product Name Alternative

E5555; ER-172594-00

UNSPSC

12352005

Target

Apoptosis; JAK; Protease Activated Receptor (PAR)

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; GPCR/G Protein; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/atopaxar.html

Concentration

10mM

Purity

99.87

Solubility

DMSO : ≥ 100 mg/mL

Smiles

COC1=C(N2CCOCC2)C=C(C(CN(CC3=C4C(F)=C(OCC)C(OCC)=C3)C4=N)=O)C=C1C(C)(C)C

Molecular Formula

C29H38FN3O5

Molecular Weight

527.63

References & Citations

[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

PAR1

Available Sizes

Curated Selection

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