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[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID

Basic information Safety Related Supplier
[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID Basic information
[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID Chemical Properties
  • Boiling point:602.1±55.0 °C(Predicted)
  • Density 1.160
  • pka3.51±0.10(Predicted)
[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID Usage And Synthesis
  • DescriptionProstacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets. The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation. MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM. In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs. Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor. As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.
  • UsesMRE-269 an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269 is used for the treatment of pulmonary arterial hypertension. MRE-269 is an active metabolite of Selexipag (S253150).
  • DefinitionChEBI: A member of the class of pyrazines that is {4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetic acid carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. The active metabolite of selexipag, an orphan drug used for the treatm nt of pulmonary arterial hypertension.
[4-[(5,6-DIPHENYLPYRAZINYL)(1-METHYLETHYL)AMINO]BUTOXY]-ACETIC ACID(475085-57-5)Related Product Information
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