- Product NameSelexipag(NS-304)
- Brief DescriptionInhibitors
- Purification99.00%
- Biological ActivityNS-304 is an orally available and potent agonist for the PGI(2) receptor (IP receptor). The inhibition constant (K(i)) of MRE-269 for the human IP receptor was 20 nM; in contrast, the K(i) values for other prostanoid receptors were >2.6 microM. MRE-269 was therefore a highly selective agonist for the IP receptor. The plasma concentrations of MRE-269 remained near peak levels for more than 8 h after oral administration of NS-304 to rats and dogs, and NS-304 increased femoral skin blood flow in rats in a long-lasting manner without affecting the hemodynamics. These findings indicate that NS-304 acts as a long-acting IP receptor agonist in vivo. The continuous vasodilation evoked by NS-304 was not attenuated by repeated treatment, indicating that NS-304 is unlikely to cause severe desensitization of the IP receptor in rats.
- Target NameOthers agonist
- CAS No. 475086-01-2
- Calculated MW 496.62
- Formulation C26H32N4O4S
- Storage 3 years -20˚C powder;2 years -80˚C in solvent;
