Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs

Iloprost – 5 mg

Brand:
Cayman
CAS:
78919-13-8
Storage:
-20
UN-No:
Non-Hazardous - 1231 / 3

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.{3347} Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM.{8322} Iloprost constricts the isolated guinea pig ilium and fundus circular smooth muscle (an EP1 receptor preparation) as strongly as prostaglandin E2 (PGE2) itself.{3412} Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM.{3347} In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time.{680} It has been evaluated in several human clinical studies as a treatment for idiopathic pulmonary hypertension.{9656,10375} 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.  

 

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Description

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.{3347} Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM.{8322} Iloprost constricts the isolated guinea pig ilium and fundus circular smooth muscle (an EP1 receptor preparation) as strongly as PGE2 itself.{3412} Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets with an ED50 of about 13 nM.{3347} In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time.{680} It has been evaluated in several human clinical studies as a treatment for idiopathic pulmonary hypertension.{9656,10375} 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: 6,9α-methylene-11α,15S-dihydroxy-16-methyl-prosta-5E,13E-dien-18-yn-1-oic acid

Synonyms:  Ciloprost

Molecular weight: 360.5

CAS: 78919-13-8

Purity: ≥97%

Formulation: A solution in methyl acetate

Product Type|Biochemicals|Lipids|Prostaglandins||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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