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. 2019 Nov 22;35(1):227–234. doi: 10.1080/14756366.2019.1693555

Table 5.

In vitro microsomal stability and cytochrome P450 (CYP) inhibition assay of compound 17a.

  Microsomal stability, (%)a
CYPs enzyme inhibition, IC50 (μM)b
No Human Dog Rat Mouse CYP3A4 CYP1A2 CYP2C9 CYP2C19 CYP2D6
17a 94 82 87 82 16.2 10.6 2.9 >20 8.7
a

Remaining percent of metabolism by incubation of the parent molecule (5 μM) with liver microsomes of mouse, rat, dog, and human for 60 min (duplicate).

b

Data were analysed by a fluorescence detection method.