Oatp | Substrate | Parameter | BSP | Rifamycin SV | Quinine | Rifampin | Ibuprofen | Olmesartan | Digoxin |
---|---|---|---|---|---|---|---|---|---|
1a1 | RSV | IC50 (µM) | 3.00 ± 0.25 | 3.33 ± 0.28 | 72.8 ± 6.5 | 110 ± 7 | 485 ± 52 | 612 ± 43 | NI |
H | 1.12 ± 0.06 | 1.08 ± 0.09 | 0.826 ± 0.057 | 1.63 ± 0.12 | 1.23 ± 0.19 | 0.787 ± 0.090 | ND | ||
1a4 | RSV | IC50 (µM) | 6.24 ± 1.07 | 20.5 ± 2.9 | 1.89 ± 0.31 | 1.31 ± 0.23 | NI | NI | 0.107 ± 0.015 |
H | 0.687 ± 0.087 | 0.746 ± 0.074 | 0.572 ± 0.048 | 0.704 ± 0.074 | ND | ND | 0.575 ± 0.048 | ||
1b2 | RSV | IC50 (µM) | 0.397 ± 0.040 | 0.140 ± 0.007 | 125 ± 19 | 1.12 ± 0.68 | 48.5 ± 5.1 | 23.1 ± 4.0 | NI |
H | 0.938 ± 0.078 | 1.26 ± 0.06 | 0.836 ± 0.127 | 0.752 ± 0.032 | 0.622 ± 0.042 | 0.930 ± 0.107 | ND | ||
1b2 | OLM | IC50 (µM) | 0.210 ± 0.050 | 0.088 ± 0.009 | 150 ± 30 | 0.583 ± 0.053 | 61.4 ± 13.0 | ND | NI |
H | 1.28 ± 0.29 | 1.44 ± 0.18 | 0.745 ± 0.178 | 0.835 ± 0.063 | 0.656 ± 0.119 | ND | ND |
H, Hill coefficient; ND, not determined; NI, not inhibited by 100 µM digoxin or 1000 µM.