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Description: Selective prostacyclin IP1 receptor agonist
Alternative Names: NS-304, ACT-293987
Chemical Name: 2-[4-[(5,6-Diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-N-(methylsulfonyl)acetamide
Purity: ≥98% (HPLC)
Biological Activity for Selexipag
Selexipag is a 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 269. 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 for Selexipag
Selexipag is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Selexipag
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Selexipag
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.66 | 100 |
Preparing Stock Solutions for Selexipag
The following data is based on the product molecular weight 496.62. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for Selexipag
References for Selexipag
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Selexipag, please let us know.
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