NS-304 - CAS 475086-01-2
Catalog number: 475086-01-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C26H32N4O4S
Molecular Weight:
496.6
COA:
Inquire
Targets:
Prostanoid Receptor
Description:
NS-304 is a selective prostacyclin IP1 receptor agonist as prodrug of the active form of MRE-269 with a Ki value of 20 nM.
Purity:
≥95%
Appearance:
Yellow solid
Synonyms:
Selexipag; NS-304; NS304; NS 304; ACT-293987; ACT293987; ACT 293987; 2-[4-[(5,6-Diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-N-(methylsulfonyl)acetamide;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
Selective prostacyclin IP1 receptor agonist
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
QXWZQTURMXZVHJ-UHFFFAOYSA-N
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)
Canonical SMILES:
CC(C)N(CCCCOCC(=O)NS(=O)(=O)C)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
Current Developer:
Actelion Pharmaceuticals; Nippon Shinyaku
1.Selexipag for the Treatment of Pulmonary Arterial Hypertension.
Sitbon O, Channick R, Chin KM, Frey A, Gaine S, Galiè N, Ghofrani HA, Hoeper MM, Lang IM, Preiss R, Rubin LJ, Di Scala L, Tapson V, Adzerikho I, Liu J, Moiseeva O, Zeng X, Simonneau G, McLaughlin VV; GRIPHON Investigators. N Engl J Med. 2015 Dec 24;373(26):2522-33. doi: 10.1056/NEJMoa1503184.
BACKGROUND: In a phase 2 trial, selexipag, an oral selective IP prostacyclin-receptor agonist, was shown to be beneficial in the treatment of pulmonary arterial hypertension.
2.Selexipag: First Global Approval.
Scott LJ1. Drugs. 2016 Mar;76(3):413-8. doi: 10.1007/s40265-016-0549-4.
Selexipag (Uptravi(®)) is a highly selective, long-acting, nonprostanoid, prostacyclin receptor agonist that is being developed by Actelion Pharmaceuticals Ltd and Nippon Shinyaku. Oral selexipag is approved in the USA for the treatment of pulmonary arterial hypertension (PAH; WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH. It has subsequently been approved in Canada for the long-term treatment of PAH, and received a positive opinion in the EU for the treatment of PAH in adult patients with WHO functional class II-III. Selexipag received orphan drug designation for the treatment of PAH in Japan in 2014 and is in undergoing regulatory review in several countries for use in this indication. In the large, event-driven, phase III GRIPHON trial, selexipag reduced the risk of the primary composite endpoint of death or a complication related to PAH (whichever occurred first) by 40 % compared with placebo in patients with PAH (80 % were also receiving stable dosages of an endothelin receptor antagonist and/or a phosphodiesterase 5 inhibitor).
3.Selexipag (Uptravi) for pulmonary arterial hypertension.
Med Lett Drugs Ther. 2016 Feb 15;58(1488):21-3.
4.Pharmacokinetics of the novel oral prostacyclin receptor agonist selexipag in subjects with hepatic or renal impairment.
Kaufmann P1, Cruz HG1, Krause A1, Ulč I2, Halabi A3, Dingemanse J1. Br J Clin Pharmacol. 2016 Apr 7. doi: 10.1111/bcp.12963. [Epub ahead of print]
AIM: To explore the effect of hepatic or renal dysfunction on the pharmacokinetics (PK), tolerability, and safety of selexipag, an orally active prostacyclin receptor agonist.
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CAS 475086-01-2 NS-304

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