TABLE 2

IC50 and Hill coefficient of inhibitors of organic anion transporting polypeptide (Oatp)–mediated uptake of rosuvastatin (RSV) or olmesartan acid (OLM)

These parameters were estimated using the data in Fig. 4 and Supplemental Fig. 3. The data represent the mean ± S.E. estimated by Phoenix.

OatpSubstrateParameterBSPRifamycin SVQuinineRifampinIbuprofenOlmesartanDigoxin
1a1RSVIC50 (µM)3.00 ± 0.253.33 ± 0.2872.8 ± 6.5110 ± 7485 ± 52612 ± 43NI
H1.12 ± 0.061.08 ± 0.090.826 ± 0.0571.63 ± 0.121.23 ± 0.190.787 ± 0.090ND
1a4RSVIC50 (µM)6.24 ± 1.0720.5 ± 2.91.89 ± 0.311.31 ± 0.23NINI0.107 ± 0.015
H0.687 ± 0.0870.746 ± 0.0740.572 ± 0.0480.704 ± 0.074NDND0.575 ± 0.048
1b2RSVIC50 (µM)0.397 ± 0.0400.140 ± 0.007125 ± 191.12 ± 0.6848.5 ± 5.123.1 ± 4.0NI
H0.938 ± 0.0781.26 ± 0.060.836 ± 0.1270.752 ± 0.0320.622 ± 0.0420.930 ± 0.107ND
1b2OLMIC50 (µM)0.210 ± 0.0500.088 ± 0.009150 ± 300.583 ± 0.05361.4 ± 13.0NDNI
H1.28 ± 0.291.44 ± 0.180.745 ± 0.1780.835 ± 0.0630.656 ± 0.119NDND
  • H, Hill coefficient; ND, not determined; NI, not inhibited by 100 µM digoxin or 1000 µM.