货号 | 18215-10mg |
描述 | Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin.1 Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM.2 Iloprost constricts the isolated guinea pig ilium and fundus circular smooth muscle (an EP1 receptor preparation) as strongly as prostaglandin E2(PGE2) itself.3 Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM.1 In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time.4 It has been evaluated in several human clinical studies as a treatment for idiopathic pulmonary hypertension.5,6 In these studies, an aerosolized dose of 30 µg/day was effective, and doses as high as 150 µg/day for up to a year were well tolerated. |
别名 | Ciloprost; |
供应商 | Cayman |
应用文献 | |
1.Schrör, K.,Darius, H.,Matzky, R., et al. The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK36374) - equipotent to PGI2 in vitro. Naunyn-Schmiedebergs Archives of Pharmacology 316, 252-255 (1981). 2.Abramovitz, M.,Adam, M.,Boie, Y., et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochimica et Biophysica Acta 1483, 285-293 (2000). 3.Sheldrick, R.L.G.,Coleman, R.A., and Lumley, P. Iloprost - a potent EP1- and IP-receptor agonist. British Journal of Pharmacology 94, 334P (1988). 4.Schering, A.G. Ciloprost. Drugs of the Future 7, 839-977 (1982). 5.Hoeper, M.M.,Schwarze, M.,Ehlerding, S., et al. Long-term treatment of primary pulmonary hypertension with aerosolized iloprost, a prostacyclin analogue. New England Journal of Medicine 342, 1866-1870 (2000). 6.Olschewski, H.,Simonneau, G.,Galié, N., et al. Inhaled iloprost for severe pulmonary hypertension. New England Journal of Medicine 347(5), 322-329 (2002). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥97% |
计算分子量 | 360.5 |
分子式 | C22H32O4 |
CAS号 | 78919-13-8 |
稳定性 | ≥ 1 year |
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