TABLE 1.
ADME property | Value(s) |
---|---|
Solubility | 465 μM at pH 7.4 |
Cytochrome P450 inhibition | CYPs 1A2, 2C9, 2C19, 3A4, 2D6 (IC50 >50 μM) |
Mouse liver microsome properties | t1/2, 47.8 min; CLint, 14.5 μl/min/mg protein |
Mouse plasma protein binding | 61.4% |
Mouse plasma stability (at 5 h) | 95.2% |
Human plasma protein binding | 52% |
Human plasma stability (at 5 h) | 94.8% |
Caco-2 permeability | Papp A-B, 20.4 × 10−6 cm/s; Papp B-A, 8.87 × 10−6 cm/s; efflux ratio, 0.435 |