Category IIB2 and IIB3: transported substrates (YYN/YNY)
| Compound Name | Papp A → B | Mass Balance A → B | Papp B → A | Mass Balance B → A | BA/AB Ratio | Effluxed (Y/N) | ATPase Assay Ratio | ATPase Activator (Y/N) | Calcein-AM Assay | Calcein-AM Inhibitor (Y/N) |
|---|---|---|---|---|---|---|---|---|---|---|
| nm/s | nm/s | % max | ||||||||
| Clarythromycin | 10.8 ± 0.57 | 87.2 | 336 ± 2.70 | 95.4 | 31.3 | Y | 3.55 | Y | 2.71 | N |
| Eletriptan | 18.4 ± 0.63 | 99.5 | 578 ± 18.6 | 98.3 | 31.5 | Y11-a | 2.22 | Y | 2.60 | N |
| Emetine | 9.61 ± 1.09 | 79.0 | 281 ± 42.5 | 87.3 | 29.2 | Y | 2.54 | Y | 3.39 | N |
| Erythromycin | 0.94 ± 0.12 | 88.5 | 13.5 ± 1.11 | 96.2 | 14.4 | Y11-a | 2.27 | Y | 4.35 | N |
| Indinavir | 8.69 ± 1.49 | 77.9 | 176 ± 16.0 | 80.8 | 20.3 | Y11-a | 9.59 | Y | 0.14 | N |
| Taxol | <1.2511-b | 89.2 | 135 ± 17.1 | 87.6 | >108 | Y | 2.63 | Y | 0.98 | N |
| Trimethoprim | 73.9 ± 7.45 | 85.6 | 267 ± 19.9 | 91.1 | 3.61 | Y11-a | 3.61 | Y | 1.35 | N |
| Cyclosporin A11-c | 15.9 ± 2.96 | 65.3 | 153 ± 23.9 | 78.6 | 9.61 | Y | 0.85 | N | 98.7 | Y |
| Mean | 20.4 | 255 | 21.7 | 3.77 | 2.22 | |||||
| Median | 10.2 | 267 | 24.8 | 2.63 | 2.60 | |||||
| Minimum | 0.94 | 13.5 | 3.61 | 2.22 | 0.14 | |||||
| Maximum | 73.9 | 578 | 31.5 | 9.59 | 4.35 |
n = 8 compounds.
Y, yes; N, no.
↵11-a Run in the presence and absence of 2 μM GF120918 to confirm whether the compound is transported by Pgp.
↵11-b Compound concentrations in samples below the limit quantification (BQL). Papp value is calculated from the lowest detectable standard.
↵11-c Cyclosporin A results were not included in the mean, median, minimum, and maximum calculations.