TABLE 1

Kinetic parameters for the uptake of various compounds in dog Oatp1b4-expressing HEK293 cells

VmaxKmaVmax/Km + PdifKmbReference
OATP1B1OATP1B3OATP1B1OATP1B3
pmol · min−1 · mg protein−1μMμl · min1 · mg protein−1μM
BSP319 ± 302.72 ± 0.31117 ± 170.0364–0.30.4–3.3Kullak-Ublick et al., 2001; Y. Debori, K. Maeda, and Y. Sugiyama, unpublished dataCui et al., 2001; Kullak-Ublick et al., 2001
Pitavastatin514 ± 565.49 ± 0.7393.6 ± 16.13.00 ± 0.393.25 ± 0.44Hirano et al., 2004Hirano et al., 2004
E1S952 ± 18839.0 ± 8.524.4 ± 7.20.068 ± 0.46Tamai et al., 2001; Hirano et al., 2004
Glibenclamide24.0 ± 7.30.619 ± 0.21146.8 ± 17.70.680 ± 0.3672.44 ± 0.82Unpublished dataUnpublished data
Valsartan348 ± 327.15 ± 0.7852.8 ± 6.91.39 ± 0.2418.2 ± 5.9Yamashiro et al., 2006Yamashiro et al., 2006
E2G106 ± 216.65 ± 1.3618.2 ± 4.63.71–8.295.4–24.6Tamai et al., 2001; Hirano et al., 2004König et al., 2000; Hirano et al., 2004
Taurocholate150 ± 6613.9 ± 6.614.1 ± 7.010–33.85.8 ± 1.2Hsiang et al., 1999; Cui et al., 2001Abe et al., 2001
DHEAS608 ± 14714.5 ± 3.551.7 ± 14.421.5 ± 2.5>30Cui et al., 2001; Hsiang et al., 1999Cui et al., 2001
Olmesartan151 ± 277.82 ± 1.5423.0 ± 5.112.8–42.644.2–71.8Nakagomi-Hagihara et al., 2006; Yamada et al., 2007Nakagomi-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.