Table 2.
in vitro ADME properties
| Aqueous solubility (μM) | Plasma protein binding (% bound) | CYP inhibition* | Caco-2 permeability | Liver microsome metabolic stability (% remaining) | ||||||
|---|---|---|---|---|---|---|---|---|---|---|
| pH 4.0 | pH 7.4 | human | rat | mouse | IC50 | Efflux ratio | human | rat | mouse | |
| IHVR11029 | 296 | 292 | 74 | 68 | 77 | >10μM | 4.7 | 91 | 79 | 91 |
| IHVR17028 | 299 | 311 | 88 | 86 | 83 | >10μM | 31.7 | 42 | 27 | 59 |
| IHVR19029 | 309 | 303 | 82 | 54 | 51 | >10μM | 34.2 | 93 | 92 | 87 |
Inhibition of each of the 5 CYP isozymes with 10μM of test compounds.