Description
An IP receptor agonist and active metabolite of NS 304; binds to the IP receptor (Ki = 20 nM); increases cAMP levels in human PASMCs in a concentration-dependent manner; selective for the IP receptor over the DP receptor (IC50 = 2.6 µM), EP1, EP2, EP3, and EP4 receptors (IC50s = >10, 5.8, >10, and 4.9 µM, respectively), FP receptor (IC50 = >10 µM), and TP receptor (IC50 = >10 µM); induces vasodilation equally in both large and small isolated rat pulmonary arteries in a concentration-dependent manner; inhibits ADP-induced platelet aggregation in isolated human and rat platelet-rich plasma (IC50s = 0.21 and 10 µM, respectively); reduces PDGF-induced proliferation of primary patient-derived PASMCs from patients with CTEPH