| 货号 | 10010412-50mg |
| 描述 | Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.1 The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.2,3,4,5 MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.6 In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.6 Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3receptor.7 As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced viaEP3-mediated vasoconstriction.7 |
| 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.Murata, T.,Ushikubi, F.,Matsuoka, T., et al. Altered pain perception and inflammatory response in mice lacking prostacyclin receptor. Nature 388, 678-682 (1997). 3.Cheng, Y.,Austin, S.C.,Rocca, B., et al. Role of prostacyclin in the cardiovascular response to thromboxane A2. Science 296, 539-541 (2002). 4.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). 5.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). 6.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). 7.Kuwano, K.,Hashino, A.,Noda, K., et al. 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). | |
| 运输条件 | Dry ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 419.5 |
| 分子式 | C25H29N3O3 |
| CAS号 | 475085-57-5 |
| 稳定性 | ≥ 1 year |
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