Skip to main content
. Author manuscript; available in PMC: 2013 Nov 1.
Published in final edited form as: Pharm Res. 2012 Jul 4;29(11):3053–3063. doi: 10.1007/s11095-012-0814-5

Table II.

Drug-like Properties of Compounds II and IAT Metabolic Stability, Permeability, Solubility, and Potential Drug-drug Interactions were Evaluated. Each Value Represents the Mean from Duplicate Studies

Measurement Units II IAT positive controls (mean)
Metabolic stability
 half-life in human liver microsomes min >60 28 Verapamil (12)
Permeability
 Papp(A→B) in CaCO-2 assay 10−6 cm/s 36 99 Propranolol (19)
Aqueous solubility μg/ml >75 19 SMART-H (1.1)
Drug-drug interactions
 IC50 value for Cyp3A4 (substrate: Testosterone) μM 20 5.5 Ketoconazole (0.02)
 IC50 value for Cyp2D6 (substrate: Dextromethorhan) μM >50 34 Quinindine (0.1)
 IC50 value for Cyp2C19 (substrate: (S)-mephennytion) μM 6.6 5.3 Ticlopidine (0.37)
 IC50 value for Cyp2C9 (substrate: Diclofenac) μM 17 4.9 Sulfaphenazole (0.5)
 IC50 value for Cyp1CA2 (substrate: Phenacetin) μM 9.2 8.1 Furafylline (2.2)