Table 2. Evaluation of Aqueous Solubility, In Vitro Metabolism, and LogD for Selected Compounds.
aqueous
solubility |
liver microsomes |
hepatocytes | |||||
---|---|---|---|---|---|---|---|
cmpd | pH 7.4 (μM)a | pH 6.5 (μM)b | pH 1.2 (μM)c | mouse CLint (μL/min/mg) | human CLint (μL/min/mg) | rat CLint (μL/min/106 cells) | logDd |
17 | <1.2 | 1.5 | 4.6 | 16.2 | 12.4 | 53.8 | 2.6 |
21 | 22.9 | 205.2 | >92.4 | 3.2 | |||
41 | <1.2 | 44.1 | 101.9 | 24.7 | 4.2 | ||
43 | 10.4 | 193.2 | >92.4 | 4.6 |
Kinetic in PBS.
Kinetic FaSSIF.
Kinetic FaSSGF.
Shake-flask method.