BAY-7801 (BAY7801) is a potent, selective, and orally bioavailable PDE9A inhibitor with IC50 of 15 nM (human PDE9A), 49-fold selectivity over PDE1.
BAY-7801 also potently inhibits mouse and rat PDE9A with IC50 of 34 and 42 nM, respectively.
BAY-7801 displays >100-fold selectivity over other phosphodiesterases.
BAY-7801 showed an EC50 of 1 μM which favorably compares to 1.7 μM for PF-04447943 in cell-based assays.
BAY-7801 (10 mg/kg, 5 weeks) significantly reduced hypertrophy of the left atrium and improved the heart function in transverse aortic constriction mouse model.
