Table 1

Km and Ki values of TCA, digoxin, and E217βG for Oatp2

InhibitorSubstrate
TCADigoxinE217βG
μM
TCA K m = 187 ± 46 K i = 156 ± 23 K i = 39.4 ± 22.5
Digoxin K i = 0.58 ± 0.27 K m = 1.07 ± 0.18 K i = 0.037 ± 0.029
E217βG1-a 1-b K m= 17.0 ± 5.5

Data are taken from Fig. 2, 3, and Sugiyama et al. (2001). These Km and Kivalues were determined by nonlinear regression analysis. Each point represents the mean ± S.E. (n = 3).

  • 1-a  The uptake of TCA was stimulated in the presence of E217βG (Fig. 2).

  • 1-b  The uptake of digoxin in the presence of E217βG (100 μM) was slightly reduced to half of the control value (Fig. 2).