Iloprost (CAS 78919-13-8)
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A second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin.1 It binds with equal affinity to the human recombinant EP1 and IP 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 This compound inhibits the ADP, collagen-induced and thrombin aggregation of human platelets with an ED50 of about 13 nM.1 In whole animals, iloprost acts as a hypotensive, antidiuretic, vasodilator 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.
Iloprost (CAS 78919-13-8) References
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-Schmiedeberg's Arch Pharmacol 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. Biochim Biophys Acta 1483 285-293 (2000). 3 Sheldrick, R.L.G., Coleman, R.A., Lumley, P. Iloprost - a potent EP1- and IP-receptor agonist. Br J Pharmacol (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. N Engl J Med 342 1866-1870 (2000). 6 Olschewski, H., Simonneau, G., Galié, N., et al. Inhaled iloprost for severe pulmonary hypertension. N Engl J Med 347(5) 322-329 (2002).Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Iloprost, 500 µg | sc-205349 | 500 µg | $155.00 | |||
Iloprost, 1 mg | sc-205349A | 1 mg | $269.00 |