SGLT

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SGLTシグナル伝達経路

SGLT製品

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  • SGLT阻害剤 (15)
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S1548 Dapagliflozin Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Biomedicines, 2023, 10.3390/biomedicines11112980
Biomedicines, 2023, 11(10)2674
Biomedicines, 2023, 11(10)2674
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
J Clin Invest, 2023, 133(8)e164610
J Neuroinflammation, 2023, 20(1):296
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 Cardiovasc Med, 2023, 10:1064290
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.
Biomedicines, 2023, 10.3390/biomedicines11112980
Biomedicines, 2023, 11(10)2674
Biomedicines, 2023, 11(10)2674
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
J Clin Invest, 2023, 133(8)e164610
J Neuroinflammation, 2023, 20(1):296
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 Cardiovasc Med, 2023, 10:1064290
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.

SGLT阻害剤の選択性比較

Tags: SGLT inhibitor|SGLT agonist|SGLT activator|SGLT inducer|SGLT antagonist|SGLT signaling pathway|SGLT assay kit