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CAS No. | 475086-01-2 | Cat. No. | BCP09146 |
Name | Selexipag | ||
Synonyms | NS-304; NS304; NS 304; ACT-293987; ACT293987; ACT 293987; | ||
SMILES | |||
Chemical Name | |||
Formula | C26H32N4O4S | M. Wt | 496.62 |
Purity | 98% | Storage | Store at 4-8°C |
Description | NS-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. |
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