1229018-87-4

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6. TPN171 is a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension. TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH)[1].

PDE5: 0.62 nM (IC₅₀)

[1] Wang Z, et al. Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2019 May 23;62(10):4979-4990. DOI:10.1021/acs.jmedchem.9b00123