SGLT2 IC50 values and SGLT2 selectivity of SGLT2 inhibitors
SGLT2 selectivity is expressed as the ratio of IC50 of a compound against hSGLT1, hSGLT3, hSGLT4, hSGLT5, hSGLT6, or hSMIT1 to its IC50 against hSGLT2.
| Inhibitor | IC50 | SGLT2 Selectivity | |||||
|---|---|---|---|---|---|---|---|
| hSGLT2 | hSGLT1 | hSGLT3 | hSGLT4 | hSGLT5 | hSGLT6 | hSMIT1 | |
| nM | |||||||
| Tofogliflozin | 2.9 ± 0.7 | 2900 | 19,000 | 1500 | 540 | 6200 | 28,000 |
| Dapagliflozin | 1.3 ± 0.2 | 610 | 190,000 | 3000 | 210 | 1300 | 22,000 |
| Canagliflozin | 6.7 ± 2.9 | 290 | 52,000 | 2800 | 180 | 200 | 5600 |
| Ipragliflozin | 2.8 ± 0.5 | 860 | 7700 | 4500 | 87 | 3500 | 21,000 |
| Empagliflozin | 3.6 ± 1.6 | 1100 | 62,000 | 2200 | 110 | 1100 | 8300 |
| Luseogliflozin | 3.1 ± 0.1 | 1600 | 8100 | 9800 | 280 | 220 | 7800 |
| PF-04971729 | 1.4 ± 0.1 | 1300 | >71,000 | 2300 | 3400 | 980 | 26,000 |
| Phlorizin | 16.4 ± 5.2 | 11 | 1300 | 490 | 36 | 1000 | 25,000 |