Home Immunology & Inflammation Prostaglandin Receptor agonist Selexipag For research use only.

Selexipag

Synonyms: NS-304, ACT-293987

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).

Selexipag Chemical Structure

Selexipag Chemical Structure

CAS: 475086-01-2

Selleck's Selexipag has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

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Biological Activity

Description 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).
Targets
prostacyclin IP receptor [1]
In vitro
In vitro Selexipag is an orally available, selective IP receptor agonist. It is rapidly hydrolysed in the hepatic microsomes to an active metabolite. Selexipag and its active metabolite have a higher binding affinity for the human IP receptor than for any other prostanoid receptor[1].
In Vivo
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, Selexipag is well tolerated, with a safety profile in line with that of the expected pharmacological effect[1]. Selexipag has a half-life of 0.8-2.5 hours[2].

Chemical lnformation & Solubility

Molecular Weight 496.62 Formula

C26H32N4O4S
CAS No. 475086-01-2 SDF Download Selexipag SDF
Smiles CC(C)N(CCCCOCC(=O)NS(=O)(=O)C)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 99 mg/mL ( (199.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh 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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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