Enpp-1-IN-11 (compound 23) is a highly potent inhibitor of Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1), with a Ki value of 45 nM. It demonstrates excellent stability in human and mouse plasma and exhibits low clearance in both human and mouse liver microsomes, holding promise for anticancer research [1].

Enpp-1-IN-11 exhibits low metabolic clearance in both human and mouse liver microsomes, alongside significant plasma stability in human and mouse plasma [1]. In a study focused on its pharmacokinetic properties in female BALB/c mice [1], Enpp-1-IN-11 demonstrated when administered orally (PO) at 10 mg/kg and intravenously (IV) at 1 mg/kg, the drug reached peak plasma concentrations (C_max) of 33.10 ng/mL and 1600.20 ng/mL, respectively, with time to peak (T_max) observed at 1.2 hours (PO) and significantly quicker at 0.08 hours (IV). Initial concentrations (C_0) were notably high at 4546.51 ng/mL. The area under the curve (AUC_last and AUC_inf) also varied significantly between the two administration routes, suggesting differences in exposure, with AUC_inf standing at 31.78 ng/mL·h (PO) and 415.55 ng/mL·h (IV). The fraction of drug extrapolated beyond the last measured time point (AUC_extrap) was minor, indicating thorough sampling. Its half-life (t_1/2) and mean residence time (MRT_last) were brief, at approximately 0.54 hours and 0.66 hours for PO, and even shorter for IV. Clearance (CL) and steady-state volume of distribution (V_SS) were calculated at 40.10 mL/min/kg and 0.22 L/kg, respectively, with bioavailability (F%) being less than 1.