Atopaxar (hydrobromide)

• 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].

• Product Name Alternative:

  E5555 (hydrobromide) ; ER 172594-06

• 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

• Field of Research:

  Cancer; Cardiovascular Disease

• Assay Protocol:

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

• Solubility:

  10 mM in DMSO

• Smiles:

  COC1=C (N2CCOCC2) C=C (C (CN (CC3=C4C (F) =C (OCC) C (OCC) =C3) C4=N) =O) C=C1C (C) (C) C.[H]Br

• Molecular Formula:

  C29H39BrFN3O5

• Molecular Weight:

  608.54

• 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

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  PAR1

• CAS Number:

  474550-69-1