| 货号 | 10010411-50mg |
| 描述 | 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.1 The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.2,3,4,5,6 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.7 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.7 |
| 别名 | ACT-293987;Selexipag; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Aristoff, P.A.,Johnson, P.D. and Harrison, A.W. Synthesis of 9-substituted carbacyclin analogues. J. Org. Chem. 48, 5341-5348 (1983). 2.Southall, M.D. and Vasko, M.R. Prostaglandin receptor subtypes, EP3C and EP4, mediate the prostaglandin E2-induced cAMP production and sensitization of sensory neurons. The Journal of Biological Chemisty 276(19), 16083-16091 (2001). 3.Murata, T.,Ushikubi, F.,Matsuoka, T., et al. Altered pain perception and inflammatory response in mice lacking prostacyclin receptor. Nature 388, 678-682 (1997). 4.Cheng, Y.,Austin, S.C.,Rocca, B., et al. Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 296, 539-541 (2002). 5.Cui, Y.,Kataoka, Y.,Satoh, T., et al. Protective effect of prostaglandin I2 analogs on ischemic delayed neuronal damage in gerbils. Biochemical and Biophysical Research Communications 265, 301-304 (1999). 6.McLaughlin, V.V.,Genthner, D.E.,Panella, M.M., et al. Reduction in pulmonary vascular resistance with long-term epoprostenol (prostacyclin) therapy in primary pulmonary hypertension. New England Journal of Medicine 338, 273-277 (1998). 7.Kuwano, K.,Hashino, A.,Asaki, T., et al. 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(3), 1181-1188 (2007). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 496.6 |
| 分子式 | C26H32N4O4S |
| CAS号 | 475086-01-2 |
| 稳定性 | ≥ 1 year |
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