In Vitro: PD-166793 (0.1 μM) leads to a 20% inhibition of AMP deaminase (AMPD) activity in rat heart homogenates. PD-166793 (100 μM; 36 h) significantly reduces MMP‐9 activity in normal human cardiac fibroblasts.
In Vivo: PD-166793 (1 mg/kg/d; daily gavage for 10 weeks) largely prevents the adverse remodeling characteristically seen in the aortocaval (AV) fistula model. PD-166793 (5 mg/kg; oral gavage) exhibits superior pharmacokinetics (t1/2=43.6 h, Cmax=42.4 µg/mL, AUC0-∞=2822 µg•h/mL) in rats.