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Selexipag
- NS 304 - ACT 293987 - Uptravi
Axon 2605
CAS:
475086-01-2
Purity:
100%
- Soluble in DMSO
- MF: C26H32N4O4S
- MW: 496.62
Description
Selexipag (NS-304, ACT-293987) is an oral, long-acting prodrug of the selective prostacyclin (IP) receptor agonist MRE-269:
- Pharmacokinetics & Metabolism: Rapidly hydrolyzed by hepatic carboxylesterase 1 (CES1) into MRE-269. Selexipag has an IP receptor Ki of 260 nM, compared to the sub-nanomolar shift (Ki = 12–20 nM) of its active metabolite MRE-269.
- High Selectivity Profile: Spares traditional prostanoid receptors (EP1-EP4, DP, FP), significantly reducing standard gastrointestinal toxicities.
- Research & Disease Applications: Supports robust mechanistic studies of IP receptor pharmacology in hypertension models across biochemical, cellular, and in vivo platforms.
- Therapeutic Efficacy: Proven capable of reversing vascular endothelial dysfunction, pulmonary arterial wall hypertrophy, and right ventricular hypertrophy.
More Information
| Parent CAS No. | 475086-01-2 |
|---|---|
| Chemical Name | 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)-N-(methylsulfonyl)acetamide |
| SMILES | C(NS(C)(=O)=O)(=O)COCCCCN(C1=NC(C2=CC=CC=C2)=C(C2=CC=CC=C2)N=C1)C(C)C |
| MFCD | N.A. |
| InChi | 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 |
| CID | 9913767 |
| Short Description | IP agonist prodrug |
Selexipag (NS-304
ACT-293987)
oral
long-acting prodrug of the prostacyclin (IP) receptor agonist
Selexipag
NS-304
ACT-293987
NS 304
ACT 293987
NS304
ACT293987
Prostaglandins
PGI2 (IP)
MRE269
PGI2
oral and long-acting prodrug of the prostacyclin (IP) receptor
Agonist
prostanoid signaling
metabolism
vascular biology
hypertension
pharmacokinetics
GPCR pharmacology
receptor selectivity
receptor pharmacology
signal transduction
CAS 475086-01-2
CAS 1267423-51-7
Axon Medchem
Axon 2605
Supplier
Vendor
References
- K Kuwano et al. 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. 2007 Sep;322(3):1181-8.
- K Kuwano et al. A long-acting and highly selective prostacyclin receptor agonist prodrug, NS-304, ameliorates rat pulmonary hypertension with unique relaxant responses of its active form.... J Pharmacol Exp Ther. 2008 Sep;326(3):691-9.
- G Simonneau et al. Selexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. Eur Respir J. 2012 Oct;40(4):874-80.
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