Biological Activity
Selective prostacyclin IP1 receptor agonist (Ki values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP1-4, DP, FP, and TP receptors). Prodrug for the active form of MRE 26. Ameliorates vascular endothelial dysfunction and increases femoral skin blood flow in rats. Orally available.
Licensing Information
Sold with the permission of Nippon Shinyaku Co.
Compound Libraries
Selexipag is also offered as part of the Tocriscreen Plus and Tocriscreen Library of FDA-Approved Compounds. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 496.62 |
| Formula | C26H32N4O4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 475086-01-2 |
| PubChem ID | 9913767 |
| InChI Key | QXWZQTURMXZVHJ-UHFFFAOYSA-N |
| Smiles | CC(C)N(CCCCOCC(NS(C)(=O)=O)=O)C1=NC(C3=CC=CC=C3)=C(C2=CC=CC=C2)N=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.66 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 496.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.01 mL | 10.07 mL | 20.14 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.03 mL |
| 10 mM | 0.2 mL | 1.01 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Kuwano et al (2007) 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J.Pharmacol.Exp.Ther. 322 1181 PMID: 17545310
Kuwano et al (2008) A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active fo J.Pharmacol.Exp.Ther. 326 691 PMID: 18552131
Morrison et al (2010) Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function. J.Pharmacol.Exp.Ther. 335 249 PMID: 20660124
Keywords: Selexipag, supplier, NS304, Selexipag, agonists, prostaglandin, PGI2, analogue, IP, receptors, hypertension, vascular, supplier, NS-304, ACT-293987, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience
