Selexipag Prostaglandin Receptor agonist

Cat.No.S3726

Selexipag (NS-304, ACT-293987) is an orally active, first-in-class, selective prostacyclin IP receptor agonist with Ki value of 260 nM for human IP, whereas Ki values > 10,000 nM are measured at the other human G-protein-coupled prostanoid receptors (EP1-4, DP, FP and TP).
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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (199.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 496.62 Formula

C26H32N4O4S

Storage (From the date of receipt)
CAS No. 475086-01-2 Download SDF Storage of Stock Solutions

Synonyms NS-304, ACT-293987 SMILES CC(C)N(CCCCOCC(=O)NS(=O)(=O)C)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3

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Mechanism of Action

Targets/IC50/Ki
prostacyclin IP receptor
In vitro
Selexipag is an orally available, selective IP receptor agonist. It is rapidly hydrolysed in the hepatic microsomes to an active metabolite. This compound and its active metabolite have a higher binding affinity for the human IP receptor than for any other prostanoid receptor.
In vivo
As selexipag is rapidly hydrolysed in the liver to the active metabolite, peak-trough fluctuations in serum levels of active compound may be reduced, thereby reducing the likelihood of adverse events. Thus, this compound is well tolerated, with a safety profile in line with that of the expected pharmacological effect. It has a half-life of 0.8-2.5 hours.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-15)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07700303 NOT_YET_RECRUITING
Pulmonary Arterial Hypertension
University of Alberta
2026-09-30
NCT05825417 ACTIVE_NOT_RECRUITING
Pulmonary Arterial Hypertension
Sheffield Teaching Hospitals NHS Foundation Trust
2023-06-14 PHASE4
NCT07759804 NOT_YET_RECRUITING
Pulmonary Arterial Hypertension (PAH)
Liquidia Technologies, Inc.
2026-09 PHASE4
NCT05179876 RECRUITING
Hypertension, Pulmonary
Actelion
2022-05-04 PHASE3
NCT07694128 COMPLETED
Arterial Hypertension (PAH)
Humanis Saglık Anonim Sirketi
2026-04-08 PHASE1
NCT06932198 COMPLETED
Pulmonary Arterial Hypertension (PAH)
Humanis Saglık Anonim Sirketi
2025-01-09 PHASE1

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