Table 2.
Parameter | 4a | 4b | 4e | 4f | 8b | GAL |
---|---|---|---|---|---|---|
Mw | 459.58 | 489.60 | 503.59 | 473.60 | 523.62 | 287.35 |
pKa | 7.78 | 7.77 | 7.77 | 7.77 | 6.58 | 7.92 |
logP | 4.53 ± 0.8 | 4.48 ± 0.81 | 4.64 ± 0.85 | 4.99 ± 0.80 | 4.9 ± 0.85 | 1.75 |
logD7.4 | 3.97 | 3.92 | 4.09 | 4.43 | 4.83 | 1.12 |
PSA | 59.00 | 68.23 | 77.46 | 59.00 | 68.23 | 41.93 |
HBD | 1 | 1 | 1 | 1 | 1 | 1 |
HBA | 5 | 6 | 7 | 5 | 6 | 4 |
fBH+ | 0.71 | 0.70 | 0.70 | 0.70 | 0.13 | 0.77 |
VDssL/kg | 4.71 | 4.95 | 5.88 | 5.31 | 1.85 | 2.30 a |
fu | 0.082 | 0.085 | 0.094 | 0.078 | 0.029 | 0.83 a |
CL, L/h/kg | 0.466 | 0.412 | 0.388 | 0.445 | 0.305 | 0.336 a |
t1/2, h | 7.01 | 8.32 | 10.51 | 8.28 | 4.19 | 4.74 |
a [54].