| S1548 |
Dapagliflozin
|
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4. |
-
Cell Death Dis, 2025, 16(1):79
-
Sci Adv, 2025, 11(31):eadu3700
-
Eur Heart J, 2024, 31:ehae472.
|
|
| S2760 |
Canagliflozin (JNJ 28431754)
|
Canagliflozin (TA 7284, JNJ 28431754) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. |
-
Redox Biol, 2024, 71:103103
-
Toxicol Appl Pharmacol, 2024, 495:117183
-
J Clin Invest, 2023, 133(1)e154754
|
|
| 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
-
Biomed Pharmacother, 2024, 180:117453
-
Sci Rep, 2024, 14(1):16459
|
|
| 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
|
|
| S5901 |
Canagliflozin hemihydrate
|
Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. |
-
Front Pharmacol, 2022, 13:848310
-
Yonsei Med J, 2022, 63(7):619-631
-
Cell Death Dis, 2018, 9(2):226
|
|
| S5566 |
Dapagliflozin propanediol monohydrate
|
Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
-
J Cell Mol Med, 2025, 29(11):e70581
-
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.
|
|
|
| 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.
|
|
|
| E0910New |
Swertisin
|
Swertisin, a novel SGLT2 inhibitor, with improved glucose homeostasis for effective diabetes therapy.
|
|
|
| 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. |
- Cell Death Dis, 2025, 16(1):79
- Sci Adv, 2025, 11(31):eadu3700
- Eur Heart J, 2024, 31:ehae472.
|
|
| S2760 |
Canagliflozin (JNJ 28431754)
|
Canagliflozin (TA 7284, JNJ 28431754) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. |
- Redox Biol, 2024, 71:103103
- Toxicol Appl Pharmacol, 2024, 495:117183
- J Clin Invest, 2023, 133(1)e154754
|
|
| 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
- Biomed Pharmacother, 2024, 180:117453
- Sci Rep, 2024, 14(1):16459
|
|
| 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
|
|
| S5901 |
Canagliflozin hemihydrate
|
Canagliflozin hemihydrate is the hemihydrate form of canagliflozin, which is a SGLT2 inhibitor with IC50 of 2.2 nM for hSGLT2 in a cell-free assay, exhibits 413-fold selectivity over hSGLT1. |
- Front Pharmacol, 2022, 13:848310
- Yonsei Med J, 2022, 63(7):619-631
- Cell Death Dis, 2018, 9(2):226
|
|
| S5566 |
Dapagliflozin propanediol monohydrate
|
Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors. |
- J Cell Mol Med, 2025, 29(11):e70581
- 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.
|
|
|
| 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.
|
|
|
| E0910New |
Swertisin
|
Swertisin, a novel SGLT2 inhibitor, with improved glucose homeostasis for effective diabetes therapy.
|
|
|
| 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. |
|
|