FATP1-IN-1 is a potent inhibitor of fatty acid transport protein 1 (FATP1). It effectively inhibits the activity of recombinant human or mouse acyl-CoA synthetase, which is essential for the function of FATP1. The inhibition is characterized by IC50 values of 0.046 μM for human FATP1 and 0.60 μM for mouse FATP1.

FATP1-IN-1 administered orally (p.o.) at a dosage of 10 mg/kg demonstrated pharmacokinetic parameters with a maximum concentration (C max) of 5.5 μg/mL, an area under the curve (AUC) of 36 μg h/mL, and a time to reach maximum concentration (T max) of 0.33 hours. These results were attained in a mouse plasma [1] model and surpassed the IC 50 value of 0.22 μM for mice, without accounting for plasma protein binding.