Formulation: A solution in methyl acetate
Formal Name: 5-((3aS,4R,5R,6aS,E)-5-hydroxy-4-((3S,E)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)hexahydropentalen-2(1H)-ylidene)pentanoic-3,3,4,4-d4 acid
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C22H28D4O4
Formula Weight: 364,5
Shelf life (days): 365
Notes: Iloprost-d4 is intended for use as an internal standard for the quantification of iloprost (Item No. 18215) by GC- or LC-MS. Iloprost is an agonist of the IP receptor and the prostaglandin E2 (PGE2) receptor subtype EP1 and a derivative of PGI2.{8322,72436} It selectively binds to IP and EP1 receptors (Ki = 11 nM for both) over EP2, EP4, DP, FP, and TP receptors (Kis = 1,870, 284, 1,035, 619, and 6,487 nM, respectively) but also binds to the EP3 receptor (Ki = 56 nM).{8322} Iloprost increases cAMP levels in HEK293 cells expressing IP or EP3 receptors (EC50s = 0.37 and 27.5 nM, respectively) and increases calcium levels in HEK293 cells expressing the EP1 receptor (EC50 = 0.3 nM).{72436} It inhibits ADP-, thrombin-, and collagen-induced platelet aggregation in isolated human platelet-rich plasma (IC50s = 1.07, 0.71, and 0.24 nM, respectively).{3347} Iloprost (100 ng/kg per minute) increases the time to occlusive coronary artery thrombosis in a porcine model of electrically induced coronary artery thrombosis.{72437} Aerosolized administration of iloprost (130-1,300 ng/kg per minute) reduces right ventricular systolic pressure and reverses vascular remodeling in rats in a model of chronic pulmonary hypertension induced by the alkaloid monocrotaine (Item No. 16666).{72438} Formulations containing iloprost have been used in the treatment of pulmonary arterial hypertension and severe frostbite.
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