Table 1.
Measured Ki and K0.5 values for hSGLT2, hSGLT1 and hSGLT1 mutants
| Transporter | K0.5 αMDG (mM) | K0.5 Na+ (mM) | Ki phlorizin (μM) | Ki phloretin (μM) | Ki dapagliflozin (μM) | Ki dapa-aglycon (μM) |
|---|---|---|---|---|---|---|
| hSGLT1 | ||||||
| Wild-type | 0.9 ± 0.1 | 36 ± 1 | 0.22 ± 0.04 | 55 ± 12 | 0.45 ± 0.02 | 425 ± 50 |
| F101C | 1.1 ± 0.220 | 9 ± 120 | 37 ± 1220 | |||
| D268H | 1.2 ± 0.1 | 17 ± 1.2 | 0.3 ± 0.1 | 0.035 ± 0.011 | ||
| T287C | 1.4 ± 0.219 | 6 ± 0.219 | 0.2 ± 0.1 | |||
| Y290C | >10020 | 46 ± 520 | 36 ± 620 | |||
| Y290F | 35 ± 1021 | 20 ± 121 | 1.8 ± 0.4 | |||
| S392A/C | >10020 | 122 ± 1220 | 4 ± 120 | |||
| S393A/C | 4 ± 120 | 32 ± 320 | 0.5 ± 0.220 | |||
| T395A | 34 ± 4 | 104 ± 50 | 0.35 ± 0.10 | 20 ± 7 | 0.4 ± 0.1 | 187 ± 80 |
| Q457C | 13 ± 220 | 34 ± 220 | 6 ± 120 | |||
| F453C | 1.8 ± 0.220 | 21 ± 120 | 1 ± 0.320 | |||
| hSGLT2 | ||||||
| Wild-type | 4.4 ± 0.1 | 22 ± 1 | 0.03 ± 0.01 | 27 ± 3 | 0.004 ± 0.001 | 110 ± 30 |
All parameters were estimated from SGLT current measurement in oocytes at 22 °C and each parameter is given as the mean and ±SEM of three to five estimates. The results for wild-type hSGLT1 and hSGLT2 agree with previous reports20, 27, 65. Superscripts refer to data obtained for hSGLT1 mutants expressed in oocytes and reported previously19–21. Data reported without superscripts were generated for this study