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. 2023 Dec 6;13(50):35583–35591. doi: 10.1039/d3ra06790d

In vitro microsomal stability and plasma protein binding of representative analogs.

Compound Microsomal stability (%)a Plasma protein binding rate (%)
Mouse Human Mouse Human
8 67.7 ± 5.6 50.7 ± 3.2 84.8 ± 3.4 81.3 ± 2.0
44 15.7 ± 0.4 1.4 ± 0.1 94.3 ± 0.6 93.5 ± 0.6
47 38.6 ± 0.6 21.8 ± 1.4 89.3 ± 1.0 87.4 ± 2.4
56 50.6 ± 1.2 20.2 ± 2.3 96.0 ± 0.2 82.9 ± 0.5
a

Percentage of test compounds remaining after 30 min in mouse and human liver microsomes in the presence of NADPH (phase I stability).