TABLE 3.
Measured total and unbound concentrations of inhibitors ([I]t and [I]u, µM) in the medium ([I]med), whole-cell lysate ([I]cell), and cytosol ([I]cyt)
SCHH were treated with telmisartan (1 or 10 µM) and bosentan (0.8 or 8 µM) for 20 min in the presence of 4% BSA. Data were generated from n = 1 SCHH preparation. Unbound concentration and fu data were expressed as mean values obtained from triplicate measurements, and values in parentheses represent ranges. Total concentrations were from single measurements.
| Inhibitor | Medium | Cell Lysate | Cytosol | ||||||
|---|---|---|---|---|---|---|---|---|---|
| [I]t,med | [I]u,med | fu,med | [I]t,cell | [I]u,cell | fu,cell,inhibitor | [I]t,cyt | [I]u,cyt | fu,cyt,inhibitor | |
| Telmisartan | 1 | 0.012 (0.0098–0.014) | 0.012 (0.0098–0.0134) | 16 | 2.1 (1.6–2.5) | 0.13 (0.099–0.16) | 16 | 0.85 (0.8–0.9) | 0.053 (0.050–0.056) |
| 10 | 0.20 (0.18–0.22) | 0.02 (0.018–0.022) | 40 | 3.7 (2.7–4.8) | 0.094 (0.068–0.12) | 35 | 2.8 (1.8–3.4) | 0.080 (0.052–0.098) | |
| Bosentan | 0.8 | 0.031 (0.023–0.039) | 0.039 (0.029–0.048) | 1.9 | 0.79 (0.66–0.93) | 0.41 (0.34–0.48) | 1.7 | 0.21 (0.21–0.21) | 0.12 (0.12–0.12) |
| 8 | 0.45 (0.44–0.47) | 0.057 (0.055–0.058) | 17 | 3.8 (3.1–4.5) | 0.22 (0.18–0.26) | 14 | N/A | N/A | |
N/A, not available.