MRE-<wbr/>269

MRE-269

CAT N°: 10010412
Price:

From 54.00 45.90

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.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{5018,9805,8508,5466} 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.{14998} 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.{14998} Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.{16443} 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.{16443}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • [4-[(5,6-diphenylpyrazinyl)(1-methylethyl)amino]butoxy]-acetic acid
  • Correlated keywords
    • MRE269 prostaglandins PGI2 IP receptors inflammation NS-304 NS304 agonists vasodilator hypotensive vascular diseases atherosclerosis hypertension analogs potent selective PGs prodrugs
  • Product Overview:
    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.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{5018,9805,8508,5466} 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.{14998} 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.{14998} Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.{16443} 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.{16443}

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