Permeability and transport of reference compounds over 20 passages
| Compound | Papp A → B | PappB → A | B → A/A → B Ratio |
|---|---|---|---|
| nm/s | |||
| Amprenavir | 37.3 ± 6.96 | 987 ± 123 | 27.7 ± 2.90 |
| Amprenavir +GF120918 | 341 ± 39.9 | 409 ± 52.1 | 1.19 ± 0.04 |
| Mannitol | 11.3 ± 2.71 | 9.15 ± 2.97 | 0.82 ± 0.18 |
| Mannitol + GF120918 | 11.3 ± 2.59 | 9.24 ± 3.27 | 0.81 ± 0.17 |
| Propranolol | 496 ± 51.2 | 514 ± 43.0 | 1.04 ± 0.09 |
| Propranolol +GF120918 | 504 ± 38.7 | 507 ± 36.6 | 1.01 ± 0.11 |
Data are reported as the average Papp ± standard deviation from seven independent transport experiments, each withn = 3 Transwells. MDR1-MDCKII cells used in studies were between passage numbers 30 and 50. Involvement of a Pgp-mediated efflux mechanism is suggested if the BA/AB ratio is >2.0. GF120918 at 2 μM was added to both donor and receiver compartments.