| S8939 |
Mizagliflozin (KWA 0711) |
Mizagliflozin (KWA 0711) is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation. |
Selective |
human SGLT1, Ki: 27 nM |
| S8938 |
KGA-2727 |
KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models. |
Selective |
human SGLT1, Ki: 97.4 nM; rat SGLT1, Ki: 43.5 nM |
| S8103 |
Sotagliflozin |
Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
|
Pan |
SGLT1, IC50: 36 nM |
| S2343 |
Phlorizin |
Phlorizin (Phloridzin) is a dihydrochalcone found in the bark of pear (Pyrus communis), apple, cherry and other fruit trees. Phlorizin is a non-selective SGLT inhibitor with Ki of 300 nM and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. |
Pan |
hSGLT1, Ki: 300 nM |
| S0993 |
Remogliflozin etabonate (GSK189075) |
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models. |
Pan |
hSGLT1, Ki: 43100 nM |
| S2342 |
Phloretin (RJC 02792) |
Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes. |
Pan |
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