TABLE 1.
Compound | hOAT1a
|
hOAT3a
|
||||
---|---|---|---|---|---|---|
Km (μM) | Vmax (pmol/min/106 cells) | Vmax/Km | Km(μM) | Vmax (pmol/min/106 cells) | Vmax/Km | |
GS-9148 | 259 ± 102 | 7.8 ± 0.8 | 0.03 | 1,216 ± 8 | 19.5 ± 14.0 | 0.016 |
Cidofovir | 58.0 ± 5.7 | 103 ± 10 | 1.77 | NDb | ND | ND |
Adefovir | 23.8 ± 4.2 | 46.0 ± 4.4 | 1.93 | 1,220 ± 740 | 131.4 | 0.105 |
Tenofovir | 33.8 ± 3.4 | 110 ± 12 | 3.26 | 770 ± 210 | 28.7 ± 8.6 | 0.037 |
Data represent mean ± standard deviations from two independent experiments performed in duplicate.
ND, not determined. Cidofovir has been shown not to be a substrate for hOAT3.