WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 317125
CAS#: 475086-01-2
Description: Selexipag, also known as ACT-293987 and NS-304, is a a first-in-class orally available selective non-prostanoid IP receptor agonist, which is currently in development by Actelion as a treatment of pulmonary arterial hypertension. Selexipag and its active metabolite, ACT-333679, are agonists at the prostacyclin receptor, which leads to vasodilation in the pulmonary circulation.
MedKoo Cat#: 317125
Name: Selexipag
CAS#: 475086-01-2
Chemical Formula: C26H32N4O4S
Exact Mass: 496.21443
Molecular Weight: 496.62
Elemental Analysis: C, 62.88; H, 6.50; N, 11.28; O, 12.89; S, 6.46
Synonym: NS-304; NS304; NS 304; ACT-293987; ACT293987; ACT 293987; Selexipag; Uptravi.
IUPAC/Chemical Name: 2-{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-N-(methanesulfonyl)acetamide
InChi Key: QXWZQTURMXZVHJ-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: CC(N(CCCCOCC(NS(C)(=O)=O)=O)C1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)N=C1)C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548742/ PubMed PMID: 31644051.
2: Pharmacoeconomic Review Report: Selexipag (Uptravi) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2017 Sep. Available from http://www.ncbi.nlm.nih.gov/books/NBK533876/ PubMed PMID: 30462450.
3: Patient Group Input Submissions: selexipag (Uptravi) for Pulmonary Arterial Hypertension (WHO class II and III) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2017 Sep. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK533882/ PubMed PMID: 30462448.
4: CADTH Canadian Drug Expert Committee Final Recommendation Selexipag: (Uptravi — Actelion Pharmaceuticals Canada Inc.): Indication: Pulmonary Arterial Hypertension [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Oct 26. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK533883/ PubMed PMID: 30462441.
5: Sorensen LM, Wehland M, Kruger M, Simonsen U, Nassef MZ, Infanger M, Grimm D. A Special Focus on Selexipag - Treatment of Pulmonary Arterial Hypertension. Curr Pharm Des. 2017;23(34):5191-5199. doi: 10.2174/1381612823666170908114227. Review. PubMed PMID: 28891448.
6: Noel ZR, Kido K, Macaulay TE. Selexipag for the treatment of pulmonary arterial hypertension. Am J Health Syst Pharm. 2017 Aug 1;74(15):1135-1141. doi: 10.2146/ajhp160798. Epub 2017 May 22. Review. PubMed PMID: 28533253.
7: Honorato Pérez J. Selexipag, a selective prostacyclin receptor agonist in pulmonary arterial hypertension: a pharmacology review. Expert Rev Clin Pharmacol. 2017 Jul;10(7):753-762. doi: 10.1080/17512433.2017.1322900. Epub 2017 May 19. Review. PubMed PMID: 28524738.
8: Bruderer S, Hurst N, Remenova T, Dingemanse J. Clinical pharmacology, efficacy, and safety of selexipag for the treatment of pulmonary arterial hypertension. Expert Opin Drug Saf. 2017 Jun;16(6):743-751. doi: 10.1080/14740338.2017.1328052. Epub 2017 May 23. Review. PubMed PMID: 28494686.
9: Baker WL, Darsaklis K, Singhvi A, Salerno EL. Selexipag, an Oral Prostacyclin-Receptor Agonist for Pulmonary Arterial Hypertension. Ann Pharmacother. 2017 Jun;51(6):488-495. doi: 10.1177/1060028017697424. Epub 2017 Feb 1. Review. PubMed PMID: 28478717.
10: Duggan ST, Keam SJ, Burness CB. Selexipag: A Review in Pulmonary Arterial Hypertension. Am J Cardiovasc Drugs. 2017 Feb;17(1):73-80. doi: 10.1007/s40256-016-0209-9. Review. PubMed PMID: 27988834.
11: Hardin EA, Chin KM. Selexipag in the treatment of pulmonary arterial hypertension: design, development, and therapy. Drug Des Devel Ther. 2016 Nov 15;10:3747-3754. eCollection 2016. Review. PubMed PMID: 27895464; PubMed Central PMCID: PMC5117890.
12: Sardana M, Moll M, Farber HW. Pharmacokinetic drug evaluation of selexipag for the treatment of pulmonary arterial hypertension. Expert Opin Drug Metab Toxicol. 2016 Dec;12(12):1513-1520. Epub 2016 Nov 4. Review. PubMed PMID: 27756196.
13: Ghosh RK, Ball S, Das A, Bandyopadhyay D, Mondal S, Saha D, Gupta A. Selexipag in Pulmonary Arterial Hypertension: Most Updated Evidence From Recent Preclinical and Clinical Studies. J Clin Pharmacol. 2017 May;57(5):547-557. doi: 10.1002/jcph.834. Epub 2016 Dec 21. Review. PubMed PMID: 27670133.
14: Richter MJ, Gall H, Grimminger J, Grimminger F, Ghofrani HA. Selexipag for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2016 Sep;17(13):1825-34. doi: 10.1080/14656566.2016.1215429. Epub 2016 Aug 2. Review. PubMed PMID: 27467883.
15: Scott LJ. Selexipag: First Global Approval. Drugs. 2016 Mar;76(3):413-8. doi: 10.1007/s40265-016-0549-4. Review. PubMed PMID: 26846322.
16: Skoro-Sajer N, Lang IM. Selexipag for the treatment of pulmonary arterial hypertension. Expert Opin Pharmacother. 2014 Feb;15(3):429-36. doi: 10.1517/14656566.2014.876007. Epub 2014 Jan 7. Review. PubMed PMID: 24392948.
