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. 2022 Mar 3;13(4):665–673. doi: 10.1021/acsmedchemlett.1c00682

Figure 5.

Figure 5

Expanded profile of PLD inhibitor 34 and measurement of in vivo PLD inhibition in mice treated with 34. (A) Reduction of various PtdBuOH-d9 species by 34 in liver. (B) Selectivity and rodent PK of 34. aAverage of A-B/B-A Papp in MDCK cells with low MDR1 expression. bCYPs evaluated: 1A2, 2B6, 2D6, 2C9, 2C19, 3A4. cAverage of two experiments with n = 3 rats each. dFormulation: HPMC/Tween. (C) Liver/brain concentrations of 34 at measured time points. (D) PtdBuOH-d9 species in brains of mice treated with 34.