Compound
Liver Microsomal StabilityaT
1/2
(min)
Cellular Permeability in Caco-2 Cells
b
Plasma ProteinBindingc (% Bound at 2 µM)
Dog
Human
P
app
A→B (cm/sec × 10
-6
)
P
app
A→B (cm/sec × 10
-6
)
EffluxRatio
Dog
Human
RAL
353.9
257.1
2.8
9.5
3.4
—
—
GS-9160
43.6
26.5
1.6
6.0
3.8
93.5
89.6
GS-9224
67.1
30.2
3.8
8.8
2.3
99.5
97.7
a
Mean of 13 independent experiments.
b
Mean of 2 independent experiments.
c
Mean of 3 determinations using equilibrium dialysis.
Table 7:
In Vitro ADME Profiling of GS-9224 Relative to GS-9160 and RAL.
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