TABLE 1

GastroPlus input parameters

UK-369,003
Effective human permeability (×104 cm · s−1)2.74a
Human plasma protein binding (fup) (%)66 (0.34)
Human blood/plasma ratio1
Buffer solubility (mg/ml)
    pH 1.125
    pH 2.825
    pH 4.725
    pH 5.09.6
    pH 6.50.19
    pH 6.60.11
    pH 6.70.1
    pH 7.10.11
    pH 7.40.06
    pH 7.90.07
    pH 8.80.11
    pH 9.60.14
Fasted state simulated intestinal fluid solubility (mg/ml)0.19

  • ↵a Estimated from Caco-2 flux in the presence of P-gp inhibitors.