NS-304

• CAT Number: I003651
• CAS Number: 475086-01-2
• Molecular Formula: C26H32N4O4S
• Molecular Weight: 496.62
• Purity: ≥95%
• Synonyms: 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)-N-(methylsulfonyl)acetamide
• Target: Prostaglandin Receptor
• IUPAC Name: 2-[4-[(5,6-diphenylpyrazin-2-yl)-propan-2-ylamino]butoxy]-N-methylsulfonylacetamide
• InChI: 1S/C26H32N4O4S/c1-20(2)30(16-10-11-17-34-19-24(31)29-35(3,32)33)23-18-27-25(21-12-6-4-7-13-21)26(28-23)22-14-8-5-9-15-22/h4-9,12-15,18,20H,10-11,16-17,19H2,1-3H3,(H,29,31)
• InChIKey: QXWZQTURMXZVHJ-UHFFFAOYSA-N
• SMILES: CC(C)N(CCCCOCC(=O)NS(=O)(=O)C)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3

NS-304 (Cat No.: I003651), also known as selexipag, is a selective prostacyclin (IP) receptor agonist used to treat pulmonary arterial hypertension (PAH). It is an oral prodrug that is converted into its active metabolite, ACT-333679, which promotes vasodilation and inhibits smooth muscle cell proliferation in pulmonary arteries. By targeting the IP receptor, NS-304 improves exercise capacity and delays disease progression in PAH patients. It is generally well-tolerated, with common side effects including headache, jaw pain, nausea, and flushing. Dose titration helps manage tolerability.

Reference

1:A comparison of vasodilation mode among selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide]), its active metabolite MRE-269 and various prostacyclin receptor agonists in rat, porcine and human pulmonary arteries. Fuchikami C, Murakami K, Tajima K, Homan J, Kosugi K, Kuramoto K, Oka M, Kuwano K.Eur J Pharmacol. 2017 Jan 15;795:75-83. doi: 10.1016/j.ejphar.2016.11.057. Epub 2016 Dec 3. PMID: 27919660 2: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 form, {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid (MRE-269), on rat pulmonary artery. Kuwano K, Hashino A, Noda K, Kosugi K, Kuwabara K.J Pharmacol Exp Ther. 2008 Sep;326(3):691-9. doi: 10.1124/jpet.108.138305. Epub 2008 Jun 13. PMID: 18552131 Free Article3:2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. Kuwano K, Hashino A, Asaki T, Hamamoto T, Yamada T, Okubo K, Kuwabara K.J Pharmacol Exp Ther. 2007 Sep;322(3):1181-8. Epub 2007 Jun 1. PMID: 17545310 Free Article