SML3605
Selexipag
≥98% (HPLC)
Synonym(s):
2-{4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide, ACT-293987, NS-304
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About This Item
Empirical Formula (Hill Notation):
C26H32N4O4S
CAS Number:
Molecular Weight:
496.62
MDL number:
UNSPSC Code:
51111800
UNSPSC Code:
12352200
NACRES:
NA.21
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
SMILES string
CC(C)N(CCCCOCC(NS(C)(=O)=O)=O)C1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)N=C1
Biochem/physiol Actions
Selexipag is a potent, highly selective and orally available nonprostanoid agonist for the PGI2 receptor (IP receptor). Selexipag is readily hydrolyzed to the active metabolite ACT-333679 (MRE-269), which is also a potent and selective agonist at IP receptors. In contrast to the prostacyclin analogs iloprost and beraprost, selexipag and metabolite ACT-333679 does not contract gastric fundus up to mM concentrations.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
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A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responses of its active form, {4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}acetic acid (MRE-269), on rat pulmonary artery
Journal of Pharmacology and Experimental Therapeutics, 326(3), 691-699 (2008)
2-{4-[(5,6-Diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide (NS-304), an Orally Available and Long-Acting Prostacyclin Receptor Agonist Prodrug
Journal of Pharmacology and Experimental Therapeutics, 322, 1181-1188 (2007)
Keith Morrison et al.
The Journal of pharmacology and experimental therapeutics, 335(1), 249-255 (2010-07-28)
Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide] is an orally available prostacyclin (PGI(2)) receptor (IP receptor) agonist that is chemically distinct from PGI(2) and is in clinical development for the treatment of pulmonary arterial hypertension. Selexipag is highly selective for the human IP receptor in
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