PGI2·Na (Prostaglandin I2·Na, Prostacyclin)

PGI2·Na (Prostaglandin I2·Na, Prostacyclin) is primarily synthesized in macrovascular endothelial cells. It has been shown to induce vasodilation, inhibit platelet aggregation, as well as demonstrate fibrinolytic and cytoprotective activity. PGI2 binding to the G-protein coupled IP₁ receptor (PGI2 receptor), is believed to be responsible for the inhibition of platelet aggregation and vasodilation activity. PGI2 greatly increases cAMP concentrations, it is 30 times more active than PGE1(sc-201223), and 10 times more active than PGD2(sc-201221); however, it is a relatively unstable eicosanoid, with a half-life of about 2 minutes under physiological conditions. Analogues such as Iloprost have been developed with superior stability and similar potency for IP receptors. PGI2·Na (Prostaglandin I2·Na, Prostacyclin) is an activator of IP Receptor and an inhibitor of TXA2R.