Vmax | Kma | Vmax/Km + Pdif | Kmb | Reference | |||
---|---|---|---|---|---|---|---|
OATP1B1 | OATP1B3 | OATP1B1 | OATP1B3 | ||||
pmol · min−1 · mg protein−1 | μM | μl · min−1 · mg protein−1 | μM | ||||
BSP | 319 ± 30 | 2.72 ± 0.31 | 117 ± 17 | 0.0364–0.3 | 0.4–3.3 | Kullak-Ublick et al., 2001; Y. Debori, K. Maeda, and Y. Sugiyama, unpublished data | Cui et al., 2001; Kullak-Ublick et al., 2001 |
Pitavastatin | 514 ± 56 | 5.49 ± 0.73 | 93.6 ± 16.1 | 3.00 ± 0.39 | 3.25 ± 0.44 | Hirano et al., 2004 | Hirano et al., 2004 |
E1S | 952 ± 188 | 39.0 ± 8.5 | 24.4 ± 7.2 | 0.068 ± 0.46 | Tamai et al., 2001; Hirano et al., 2004 | ||
Glibenclamide | 24.0 ± 7.3 | 0.619 ± 0.211 | 46.8 ± 17.7 | 0.680 ± 0.367 | 2.44 ± 0.82 | Unpublished data | Unpublished data |
Valsartan | 348 ± 32 | 7.15 ± 0.78 | 52.8 ± 6.9 | 1.39 ± 0.24 | 18.2 ± 5.9 | Yamashiro et al., 2006 | Yamashiro et al., 2006 |
E2G | 106 ± 21 | 6.65 ± 1.36 | 18.2 ± 4.6 | 3.71–8.29 | 5.4–24.6 | Tamai et al., 2001; Hirano et al., 2004 | König et al., 2000; Hirano et al., 2004 |
Taurocholate | 150 ± 66 | 13.9 ± 6.6 | 14.1 ± 7.0 | 10–33.8 | 5.8 ± 1.2 | Hsiang et al., 1999; Cui et al., 2001 | Abe et al., 2001 |
DHEAS | 608 ± 147 | 14.5 ± 3.5 | 51.7 ± 14.4 | 21.5 ± 2.5 | >30 | Cui et al., 2001; Hsiang et al., 1999 | Cui et al., 2001 |
Olmesartan | 151 ± 27 | 7.82 ± 1.54 | 23.0 ± 5.1 | 12.8–42.6 | 44.2–71.8 | Nakagomi-Hagihara et al., 2006; Yamada et al., 2007 | Nakagomi-Hagihara et al., 2006; Yamada et al., 2007 |
↵a Data shown in Fig. 2 were used to determine these kinetic parameters calculated by nonlinear regression analysis as described under Materials and Methods. Each parameter represents the mean ± computer-calculated S.D.
b Values represent the mean ± computer-calculated S.D. or the range of Km values of human OATP1B1 and OATP1B3 reported previously.