Ralinepag is a prostaglandin I2 (PGI2) receptor (IP) agonist (Ki = 3 nM).1 It is selective for IP over the PGD2 receptor (DP1) and the PGE2 receptor subtypes EP1-4 (Kis = 2,600, 9,600, 611, 143, and 678 nM, respectively, in radioligand binding assays). Ralinepag induces cAMP accumulation in CHO-K1 cells expressing human recombinant IP (EC50 = 8.5 nM). In vivo, ralinepag (30 mg/kg) prevents increases in pulmonary arterial pressure and vessel wall thickness in a rat model of monocrotaline-induced pulmonary arterial hypertension.
1.Tran, T.-A., Kramer, B., Shin, Y.-J., et al.Discovery of 2-(((1r,4r)-4-(((4-chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralingepag): An orally active prostacyclin receptor agonist for the treatment of pulmonary arterial hypertensionJ. Med. Chem.60(3)913-927(2017)