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. Author manuscript; available in PMC: 2018 Sep 1.
Published in final edited form as: Exp Parasitol. 2017 Jan 5;180:71–83. doi: 10.1016/j.exppara.2017.01.001

Table 1.

Solubility (in Phosphate-Buffered Saline, pH = 6.5) and PK Properties of the BKIs. All PK parameters obtained after the inhibitors were dosed at 10 mg/kg P.O. to Mice with the exception of fecal concentrations where mice were dosed at 25 mg/kg.

Compound Solubility (μM) Tmax (hr) Cmax (μM) Plasma Protein Binding (%) AUC (μM*hr) t1/2 (hrs) Oral (mL/min/kg) Clearance Fecal Concentration (μM)
BKI-1294 82 2 0.8 84 5 3.8 80 4.4
BKI-1553 >100 5 12.8 90 402 20.0 1 0.5
BKI-1517 21 1 9.9 65 41 1.4 12 0.5