Table 5.
Physico-chemical and in vitro properties of RARβ agonist 10.
| LogDa 7.4 | Solubilityb µM pH 7.4 | MDCKc Papp × 10−6 cm/s | MDCKc asymmetry ratio | Cyp450d IC50 μM | Human Clinte µL/min/mg protein |
|---|---|---|---|---|---|
| 2.8 | >100 | 28 | 0.8 | >25 | <1 |
a
Measured by shake flask method.
b
As the amorphous sodium salt.
c
MDR1-MDCK cell line.
d
Cyp450 inhibition profile for isoforms 1A2, 2C9, 2C19, 2D6, 3A4.
e
Human microsomes incubated with the test compound at 37 °C in the presence of the co-factor, NADPH. The data is the mean on 5 separate experiments. Compound disappearance monitored over 45 min period. SEM is less than 10% of the mean values. For a–e See Ref. 9.