SGLT2
SGLT2 (SLC5A2) is a renal sodium-glucose cotransporter that mediates glucose reabsorption in the early proximal tubule and accounts for most kidney glucose reabsorption[1]. Mechanistically, renal glucose handling depends on coordinated SGLT2, SGLT1, and GLUT2 transport, linking filtered glucose recovery to sodium-coupled epithelial transport[2]. In Sglt2 knockout mice, reduced proximal tubular glucose reabsorption produced a glucosuric phenotype that models human SLC5A2-associated renal glucosuria[1]. Compared with SGLT1, SGLT2 shows low-affinity, high-capacity transport in the early proximal tubule, whereas SGLT1 provides higher-affinity, lower-capacity transport for remaining luminal glucose[2]. Therefore, SGLT2 inhibitors provide experimental tools to block renal glucose reabsorption and investigate hyperglycemia, diabetic kidney physiology, and cardiorenal outcomes[3][4][5].- Empagliflozin reduced cardiovascular death in high-risk type 2 diabetes clinical trials[4]. - Dapagliflozin reduced kidney disease progression or cardiovascular death in chronic kidney disease[5].
References:
- [1]. Vallon V, et al. SGLT2 mediates glucose reabsorption in the early proximal tubule. J Am Soc Nephrol. 2011 Jan;22(1):104-12. [Content Brief]
- [2]. Ghezzi C, et al. Physiology of renal glucose handling via SGLT1, SGLT2 and GLUT2. Diabetologia. 2018 Oct;61(10):2087-2097. [Content Brief]
- [3]. Vallon V, et al. Targeting renal glucose reabsorption to treat hyperglycaemia: the pleiotropic effects of SGLT2 inhibition. Diabetologia. 2017 Feb;60(2):215-225. [Content Brief]
- [4]. Zinman B, et al. Empagliflozin, Cardiovascular Outcomes, and Mortality in Type 2 Diabetes. N Engl J Med. 2015 Nov 26;373(22):2117-28. [Content Brief]
- [5]. Heerspink HJL, et al. Dapagliflozin in Patients with Chronic Kidney Disease. N Engl J Med. 2020 Oct 8;383(15):1436-1446. [Content Brief]
All Product Categories
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SGLT2 Related Products (67)
Related Products (67)
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Empagliflozin
0 ImagesSynonyms: BI 10773Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.
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Dapagliflozin
0 ImagesSynonyms: BMS-512148Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin induces HIF1 expression and attenuates renal IR injury.
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Phloretin
0 ImagesPhloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill.，has anti-inflammatory activities. Phloridzin is a specific，competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM，respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation.
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Phlorizin
0 ImagesPhlorizin (Floridzin) is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities.
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Bexagliflozin
0 ImagesSynonyms: EGT1442; EGT0001442; THR-1442Bexagliflozin (EGT1442) is an orally active and selective SGLT2 inhibitor with IC50 values of 0.002 μM and 5.6 μM for SGLT2 and SGLT1, respectively. Bexagliflozin selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin reduces blood glucose and HbA1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin can be used for the research of type 2 diabetes mellitus, hypertensive stroke.
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Dapagliflozin keto impurity
0 ImagesSynonyms: Oxo-dapagliflozinDapagliflozin keto impurity (Oxo-dapagliflozin) is a metabolite and impurity of Dapagliflozin (HY-10450). Dapagliflozin (BMS-512148) is a competitive inhibitor of sodium-glucose cotransporter 2 (SGLT2).
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Sotagliflozin
0 ImagesSynonyms: LX-4211; LP-802034Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.
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Ipragliflozin
0 ImagesSynonyms: ASP1941
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Dapagliflozin ((2S)-1,2-propanediol, hydrate)
0 ImagesSynonyms: BMS-512148 (2S)-1,2-propanediol, hydrateDapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury.
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Empagliflozin (Standard)
0 ImagesSynonyms: BI 10773 (Standard)Empagliflozin (Standard) is the analytical standard of Empagliflozin. This product is intended for research and analytical applications. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.
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Henagliflozin
0 ImagesSynonyms: SHR3824
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Tofogliflozin hydrate
0 ImagesSynonyms: CSG-452 hydrateTofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC50 of 2.9 nM and Ki values of 2.9 nM, 14.9 nM, and 6.4 nM for human, rat, and mouse SGLT2. Tofogliflozin partially inhibits high glucose-induced reactive oxyen species (ROS) generation in tubular cells.
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Ertugliflozin L-pyroglutamic acid
0 ImagesSynonyms: PF-04971729 L-pyroglutamic acidErtugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.
