A stable analogue of prostacyclin that potently and selectively activates the IP receptor (Ki = 20 nM); the active form of the prodrug NS-398 that is stable in vivo

MRE-269 – 5 mg

Brand:
Cayman
CAS:
475085-57-5
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 10010412 - 5 mg Category:

Description

A stable analogue of prostacyclin that potently and selectively activates the IP receptor (Ki = 20 nM); the active form of the prodrug NS-398 that is stable in vivo, as plasma concentrations of MRE-269 remain near peak levels for more than eight hours; exhibits lower affinity for the vasoconstricting EP3 receptor than other IP receptor agonists.

Formal name: [4-[(5,6-diphenylpyrazinyl)(1-methylethyl)amino]butoxy]-acetic acid

Synonyms: 

Molecular weight: 419.5

CAS: 475085-57-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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