S1548 |
Dapagliflozin
|
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4. |
-
Eur Heart J, 2024, 31:ehae472.
-
Cardiovasc Diabetol, 2024, 23(1):380
-
J Cell Mol Med, 2024, 28(6):e18176
|
|
S8022 |
Empagliflozin
|
Empagliflozin is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3. |
-
Redox Biol, 2024, 69:103010
-
Arch Biochem Biophys, 2024, 754:109958
-
J Clin Invest, 2023, 133(8)e164610
|
|
S8103 |
Sotagliflozin
|
Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
|
-
Cell Rep, 2024, 43(2):113675
-
Front Endocrinol (Lausanne), 2023, 14:1069715
-
Front Endocrinol (Lausanne), 2023, 14:1069715
|
|
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. |
-
Mol Ther Methods Clin Dev, 2022, 24:11-19
-
J Ginseng Res, 2022, 46(5):700-709
-
J Med Virol, 2019, 91(8):1440-1447
|
|
S2342 |
Phloretin (RJC 02792)
|
Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes. |
-
Br J Pharmacol, 2022, 10.1111/bph.15896
-
Food Funct, 2020, 10.1039/d0fo02362k
-
J Med Virol, 2019, 91(8):1440-1447
|
|
S5566 |
Dapagliflozin propanediol monohydrate
|
Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
-
Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
|
|
S8558 |
Tofogliflozin(CSG 452)
|
Tofogliflozin (CSG 452) is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and Hsglt1, respectively.
|
|
|
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. |
|
|
S0994 |
Ipragliflozin L-Proline
|
Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively. |
|
|
S8637 |
Ipragliflozin (ASP1941)
|
Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1.
|
|
|
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. |
|
|
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. |
|
|
S5413 |
Ertugliflozin
|
Ertugliflozin (MK-8835, PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1. |
|
|
E0141 |
Bexagliflozin (EGT1442)
|
Bexagliflozin (EGT1442, EGT-0001442, THR-1442) is a potent and selective SGLT2 inhibitor with an IC50 of 2 nM. |
|
|
S4431 |
Ertugliflozin L-pyroglutamic acid
|
Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of type 2 diabetes mellitus. |
|
|
S1548 |
Dapagliflozin
|
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4. |
- Eur Heart J, 2024, 31:ehae472.
- Cardiovasc Diabetol, 2024, 23(1):380
- J Cell Mol Med, 2024, 28(6):e18176
|
|
S8022 |
Empagliflozin
|
Empagliflozin is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3. |
- Redox Biol, 2024, 69:103010
- Arch Biochem Biophys, 2024, 754:109958
- J Clin Invest, 2023, 133(8)e164610
|
|
S8103 |
Sotagliflozin
|
Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
|
- Cell Rep, 2024, 43(2):113675
- Front Endocrinol (Lausanne), 2023, 14:1069715
- Front Endocrinol (Lausanne), 2023, 14:1069715
|
|
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. |
- Mol Ther Methods Clin Dev, 2022, 24:11-19
- J Ginseng Res, 2022, 46(5):700-709
- J Med Virol, 2019, 91(8):1440-1447
|
|
S2342 |
Phloretin (RJC 02792)
|
Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes. |
- Br J Pharmacol, 2022, 10.1111/bph.15896
- Food Funct, 2020, 10.1039/d0fo02362k
- J Med Virol, 2019, 91(8):1440-1447
|
|
S5566 |
Dapagliflozin propanediol monohydrate
|
Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
- Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
|
|
S8558 |
Tofogliflozin(CSG 452)
|
Tofogliflozin (CSG 452) is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and Hsglt1, respectively.
|
|
|
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. |
|
|
S0994 |
Ipragliflozin L-Proline
|
Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively. |
|
|
S8637 |
Ipragliflozin (ASP1941)
|
Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1.
|
|
|
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. |
|
|
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. |
|
|
S5413 |
Ertugliflozin
|
Ertugliflozin (MK-8835, PF-04971729) is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1. |
|
|
E0141 |
Bexagliflozin (EGT1442)
|
Bexagliflozin (EGT1442, EGT-0001442, THR-1442) is a potent and selective SGLT2 inhibitor with an IC50 of 2 nM. |
|
|
S4431 |
Ertugliflozin L-pyroglutamic acid
|
Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of type 2 diabetes mellitus. |
|
|