PDE5-IN-2

PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC₅₀ of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC₅₀s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity^[1]. IC50 & Target: IC50: 0.31 nM (PDE5), 1.2 nM (PDE6C), 43 nM (PDE4D2), 46 nM (PDE10A), 106 nM (PDE2A)^[1] In Vitro: PDE5-IN-2 (Compound 3) has at least 1000-fold selectivity over PDE1B, PDE3A, PDE7A1, PDE8A1, and PDE9A2 (IC₅₀s, >32 000 nM)^[1]. In Vivo: PDE5-IN-2 (1.25 mg/kg, p.o.) shows anti-pulmonary arterial hypertension activity, decreases mean pulmonary artery pressure in rats^[1].