NS-304(Selexipag)|prostacyclin receptor agonisten

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Datasheet of NS-304

Description: NS-304(Selexipag; ACT-293987) is an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. 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..

Chemical Information Catalog

DC9608

Purity of current batch:

>98%

Molecular Weight (MW)

496.62

Molecular Formula

C26H32N4O4S

CAS No.

475086-01-2

Solubility (25°C)

DMSO

Storage

Store at -20°C (desiccating conditions).

Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.


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