2-[4-[(5,6-Diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]acetic acid

Prostacyclin (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 Kivalue of 20 nM. In contrast to PGI2, which has a half-life of 30 seconds to a few minutesin vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs. Unlike the PGI2analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3receptor. As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reducedviaEP3-mediated vasoconstriction.
ChEBI: 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.