Molecular structure of NS-304, CAS Number: 475086-01-2
NS-304 (CAS 475086-01-2)
Alternate Names:
Selexipag
Application:
NS-304 is an inhibitor of human platelet aggregation
CAS Number:
475086-01-2
Molecular Weight:
496.6
Molecular Formula:
C26H32N4O4S
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
Prostaglandin I2 (PGI2) is a potent vasorelaxant and inhibitor of human platelet aggregation that mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of platelets and endothelial cells.1 The IP receptor also participates in signal transduction of the cardioprotection, inflammation and pain response.2,3,4,5,6 NS-304 is a prodrug of the active form of MRE-269, which is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.7 In contrast to PGI2, which has a half-life of 30 seconds to several minutes in vivo, NS-304 is long-acting. Plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs after NS-304 was administered orally.7
NS-304 (CAS 475086-01-2) References
- Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. | Nakamura, A., et al. 2007. Bioorg Med Chem. 15: 7720-5. PMID: 17881233
- 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., et al. 2008. J Pharmacol Exp Ther. 326: 691-9. PMID: 18552131
- Current prodrug design for drug discovery. | Hsieh, PW., et al. 2009. Curr Pharm Des. 15: 2236-50. PMID: 19601825
- A review of prostaglandin analogs in the management of patients with pulmonary arterial hypertension. | Mubarak, KK. 2010. Respir Med. 104: 9-21. PMID: 19683911
- Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat. | Tran, TA., et al. 2015. Bioorg Med Chem Lett. 25: 1030-5. PMID: 25666818
- Selexipag: An Oral and Selective IP Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. | Asaki, T., et al. 2015. J Med Chem. 58: 7128-37. PMID: 26291199
- Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. | Tran, TA., et al. 2017. J Med Chem. 60: 913-927. PMID: 28072531
- Pharmacokinetics of the selective prostacyclin receptor agonist selexipag in rats, dogs and monkeys. | Ichikawa, T., et al. 2018. Xenobiotica. 48: 186-196. PMID: 28277164
- First-in-child use of the oral selective prostacyclin IP receptor agonist selexipag in pulmonary arterial hypertension. | Geerdink, LM., et al. 2017. Pulm Circ. 7: 551-554. PMID: 28597771
- Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects. | Bruderer, S., et al. 2017. Br J Clin Pharmacol. 83: 2778-2788. PMID: 28715853
- Cross-species comparison of the metabolism and excretion of selexipag. | Ichikawa, T., et al. 2019. Xenobiotica. 49: 284-301. PMID: 29468921
- Contribution of Human Liver and Intestinal Carboxylesterases to the Hydrolysis of Selexipag In Vitro. | Imai, S., et al. 2019. J Pharm Sci. 108: 1027-1034. PMID: 30267780
- Prostaglandin I2 (PGI2) inhibits Brucella abortus internalization in macrophages via PGI2 receptor signaling, and its analogue affects immune response and disease outcome in mice. | Vu, SH., et al. 2021. Dev Comp Immunol. 115: 103902. PMID: 33091457
Inhibitor of:
IP Receptor.Activator of:
IP Receptor.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
NS-304, 1 mg | sc-205416 | 1 mg | $81.00 | |||
NS-304, 5 mg | sc-205416A | 5 mg | $339.00 |