| S8022 |
BI-10773 (Empagliflozin)
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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.
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Redox Biol, 2024, 69:103010
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Biomed Pharmacother, 2024, 180:117453
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Sci Rep, 2024, 14(1):16459
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| S2760 |
Canagliflozin (JNJ-28431754)
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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.
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Redox Biol, 2024, 71:103103
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Toxicol Appl Pharmacol, 2024, 495:117183
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J Clin Invest, 2023, 133(1)e154754
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| S1548 |
Dapagliflozin (BMS-512148)
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Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
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Cell Death Dis, 2025, 16(1):79
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Sci Adv, 2025, 11(31):eadu3700
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Eur Heart J, 2024, 31:ehae472.
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| S8103 |
Sotagliflozin (LX4211)
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Sotagliflozin is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively. Phase 3.
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Cell Rep, 2024, 43(2):113675
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Front Endocrinol (Lausanne), 2023, 14:1069715
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Front Cardiovasc Med, 2023, 10:1064290
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| S2343 |
Phlorizin
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Phlorizin (Phloridzin) is a dihydrochalcone found in the bark of pear (Pyrus communis), apple, cherry and other fruit trees. This compound is a non-selective SGLT inhibitor with Ki of 300 nM and 39 nM for hSGLT1 and hSGLT2, respectively. It is also a Na+/K+-ATPase inhibitor.
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Mol Ther Methods Clin Dev, 2022, 24:11-19
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J Ginseng Res, 2022, 46(5):700-709
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J Med Virol, 2019, 91(8):1440-1447
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| S2342 |
Phloretin (RJC 02792)
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Phloretin (RJC 02792, NSC 407292, Dihydronaringenin) is a dihydrochalcone found in apple tree leaves, and it shows beneficial effects on diabetes.
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Br J Pharmacol, 2022, 10.1111/bph.15896
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Food Funct, 2020, 10.1039/d0fo02362k
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J Med Virol, 2019, 91(8):1440-1447
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| S5901 |
Canagliflozin hemihydrate
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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.
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Front Pharmacol, 2022, 13:848310
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Yonsei Med J, 2022, 63(7):619-631
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Cell Death Dis, 2018, 9(2):226
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| S5566 |
Dapagliflozin propanediol monohydrate
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Dapagliflozin propanediol belongs to the class of orally administered antidiabetic agents designated as sodiumglucose cotransporter 2 (SGLT2) inhibitors.
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J Cell Mol Med, 2025, 29(11):e70581
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Am J Physiol Renal Physiol, 2019, 316(5):F1078-F1089
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| S8558 |
Tofogliflozin(CSG 452)
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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.
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| S0994 |
Ipragliflozin L-Proline
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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.
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