Selexipag
- CAS No.
- 475086-01-2
- Chemical Name:
- Selexipag
- Synonyms
- Selexipag;Slipper;NS-304;elexipag;Selxxipag;ACT-293987;Selexipag API;The company west;NS-304(Selexipag);Selexipag(NS-304)
- CBNumber:
- CB32454222
- Molecular Formula:
- C26H32N4O4S
- Molecular Weight:
- 496.62
- MOL File:
- 475086-01-2.mol
- Modify Date:
- 2024/7/26 15:15:00
| Melting point | 134-138°C |
|---|---|
| Density | 1.210±0.06 g/cm3(Predicted) |
| storage temp. | -20°C Freezer |
| solubility | DMSO (Slightly), Methanol (Slightly) |
| pka | 3.82±0.40(Predicted) |
| form | Solid |
| color | Pale Yellow |
| InChIKey | QXWZQTURMXZVHJ-UHFFFAOYSA-N |
| SMILES | C(NS(C)(=O)=O)(=O)COCCCCN(C1=NC(C2=CC=CC=C2)=C(C2=CC=CC=C2)N=C1)C(C)C |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313 | |||||||||
| NFPA 704 |
|
Selexipag Chemical Properties,Uses,Production
Description
Selexipag and its active metabolite, the corresponding carboxylic acid, are nonprostanoid prostaglandin I2 (PGI-2) receptor agonists. The N-methylsulfonamide within selexipag is hydrolyzed to the corresponding carboxylic acid in vivo by hepatic microsomes at a rate which provides a slow-release pharmacological effect. The compound was originally discovered by Nippon Shinyaki and later licensed to Actelion for development. The drug was approved in 2015 and first launched for the oral treatment of pulmonary arterial hypertension (PAH) in the U.S. in 2016 to delay disease progression and reduce the risk of hospitalization.
Uses
Selexipag is an orally available, highly selective, long-acting prostacyclin (IP) receptor agonist prodrug. It is a potential drug for the treatment of various vascular disorders such as pulmonary arterial hypertension and arteriosclerosis obliterans.
Definition
ChEBI: Selexipag is a member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid). It has a role as an orphan drug, a prostacyclin receptor agonist, a platelet aggregation inhibitor, a vasodilator agent and a prodrug. It is a monocarboxylic acid amide, an ether, a member of pyrazines, an aromatic amine, a tertiary amino compound and a N-sulfonylcarboxamide. It is functionally related to an ACT-333679.
Biological Activity
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 endothelial cells and platelets. The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation. Selexipag(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. In contrast to prostaglandin I2, which has a half-life of 30 seconds to a few 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.
Clinical Use
Selexipag was approved by the United States FDA on December 22, 2015 for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce risk of hospitalization.
Selective IP receptor agonist:
Treatment of pulmonary arterial hypertension.
Selexipag Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Metrochem API Private Limited | +91-4069069999 +91-4069069999 | Telangana, India | 78 | 58 | Inquiry |
| Viyash Life Sciences Pvt Ltd | +91-4023635052 +91-4023635052 | Telangana, India | 213 | 58 | Inquiry |
| Alembic Pharmaceuticals Limited | +91-2652280880 +91-2652280550 | Gujarat, India | 115 | 58 | Inquiry |
| Shilpa Medicare Limited (SML) | +91-8532238704 +91-9320649838 | Karnataka, India | 61 | 58 | Inquiry |
| Hetero Drugs Limited | +91-4023704923 +91-4023704923 | Telangana, India | 296 | 58 | Inquiry |
| Honour Lab Limited | +919845977466 | Telangana, India | 164 | 58 | Inquiry |
| Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
| Biophore India Pharmaceuticals Pvt Ltd | +91-9100031592 +91-9030907714 | Telangana, India | 134 | 58 | Inquiry |
| Symed Laboratories Ltd | +91-9505426644 +91-9505426644 | Telangana, India | 54 | 58 | Inquiry |
| Maithri Drugs Pvt Ltd | +91-9059204566 +91-9848881740 | Telangana, India | 64 | 58 | Inquiry |