Table 3.
In Vitro ADME properties for compound 35.
| Metabolic stabilitya | ||||||||
| Species | T1/2 (min) | CL int (μL/min/mg) | Remaining (T = 60min) | |||||
| RLM | 31.9 | 43.4 | 31.5% | |||||
| HLM | 45.1 | 30.7 | 42.7% | |||||
| Permeability assayb | ||||||||
| Egg-PAMPA | Mean Pe (nm/s) | Incubation Time (h) | Permeability | |||||
| – | 15.4 | 4 | High | |||||
| CYP450 inhibitionc | ||||||||
| isozyme | CYP1A2 | CYP2D6 | CYP2C9 | CYP2C19 | CYP3A4 | |||
| % inhibition | 9.8 | 13.5 | 30.6 | 25.9 | 42.6 | |||
aTestosterone and Diclofenac were used at positive control. bThe permeability assay was Performed at 10 μM concentration. High permeability: Pe > 10.0 nm/s. cPerformed at 10 μM concentration. α-Naphthoflavone (CYP1A2), Squinidine (CYP2D6), (+)-N-3-benzylnirvanol (CYP2C19), Quinidine (CYP2D6), and ketoconazole (CYP3A4) were used as the positive controls.