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. Author manuscript; available in PMC: 2017 Jul 14.
Published in final edited form as: J Med Chem. 2016 Jun 24;59(13):6512–6530. doi: 10.1021/acs.jmedchem.6b00719

Table 7.

Kinetic solubility in various media and metabolic stability in human, rat and mouse liver microsomes.

Compound Kinetic solubility (μM) pH 2 /6.5 / FaSSIF Liver microsomal species Degradation half-life (min) In vitro clearance (μL/min/mg protein) Hepatic extraction (EH)
15a 199.7 / <5 / 13 Human >150 <11.6 <0.42
Rat >150 <11.6 <0.30
Mouse >150 <11.6 <0.33

15i 197.2 / 92.7/ 153.6 Human 141.9 14.1 0.4
Rat 93.2 33.5 0.4
Mouse 52.4 130.3 0.6