Iloprost

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. Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM. Iloprost constricts the isolated guinea pig ilium and fundus circular smooth muscle (an EP1 receptor preparation) as strongly as prostaglandin E2 (PGE2) itself. Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time. It has been evaluated in several human clinical studies as a treatment for idiopathic pulmonary hypertension. 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.Formal Name: 6,9alpha-methylene-11alpha,15S-dihydroxy-16-methyl-prosta-5E,13E-dien-18-yn-1-oic acid. CAS Number: 78919-13-8. Synonyms: Ciloprost. Molecular Formula: C22H32O4. Formula Weight: 360.5. Purity: >97%. Formulation: (Request formulation change), A solution in methyl acetate. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 1 mg/ml. SMILES: O[C@@H]1C[C@H](C/2)[C@H](CC2=C\CCCC(O)=O)[C@H]1/C=C/[C@@H](O)C(C)CC#CC. InChi Code: InChI=1S/C22H32O4/c1-3-4-7-15(2)20(23)11-10-18-19-13-16(8-5-6-9-22(25)26)12-17(19)14-21(18)24/h8,10-11,15,17-21,23-24H,5-7,9,12-14H2,1-2H3,(H,25,26)/b11-10+,16-8+/t15?,17-,18+,19-,20+,21+/m0/s1. InChi Key: HIFJCPQKFCZDDL-ACWOEMLNSA-N.