Table 2. In Vitro ADME Data for 1a.
plasma protein binding (% bound) |
microsome stabilityd (% remaining) |
|||||
---|---|---|---|---|---|---|
solubility (μg/mL) pH 5.0/6.2/7.4 |
permeabilitya,bPe (× 10−6 cm/s) pH 5.0/6.2/7.4 |
human 10 μM/1 μM |
mouse 10 μM/1 μM |
plasma stabilityc (% remaining) human/mouse |
human 10 μM/1 μM |
mouse 10 μM/1 μM |
42/0.5/0.7 | 299/710/441 | 99.8/99.9 | 99.9/99.8 | 100/100 | 55/26 | 19/0.5 |
Compound at 50 μM.
PAMPA Pe: low 5 × 10−6, moderate 250 × 10−6, high 1000 × 10−6.
Plasma/PBS; compound at 40 μM, 3 h.
% remaining at 1 h.