Selective prostacyclin IP1 receptor agonists (Ki values of human and rat IP receptors are 260 and 2100 nm, and Ki values of Ep1-4, DP, FP and TP receptors are >10 μ M）。 MRE 269 prodrug in active form. Improve vascular endothelial dysfunction and increase
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
AGONIST
Mechanism of action
Prostanoid IP receptor agonist
Product Description
product 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).
1.Moncada S, Gryglewski R, Bunting S, Vane JR. (1976) An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation.. Nature, 263 (5579):(663-5). [PMID:802670]
2.Asaki T, Hamamoto T, Sugiyama Y, Kuwano K, Kuwabara K. (2007) Structure-activity studies on diphenylpyrazine derivatives: a novel class of prostacyclin receptor agonists.. Bioorg Med Chem, 15 (21):(6692-704). [PMID:17764960]
3.Sitbon O, Morrell N. (2012) Pathways in pulmonary arterial hypertension: the future is here.. Eur Respir Rev, 21 (126):(321-7). [PMID:23204120]
4.Negishi M, Sugimoto Y, Ichikawa A. (1993) Prostanoid receptors and their biological actions.. Prog Lipid Res, 32 (4):(417-34). [PMID:8309950]
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I2226059