SGLT1
SGLT1 (SLC5A1) is a sodium-glucose cotransporter that mediates intestinal D-glucose and D-galactose uptake across the brush-border membrane[1]. Mechanistically, SGLT transport uses the sodium electrochemical gradient to drive uphill glucose movement across the plasma membrane[2]. In mouse models, SGLT1 supports intestinal glucose absorption, glucose-dependent GIP and GLP-1 secretion, and about 3% of filtered renal glucose reabsorption under normoglycemia[3]. In disease relevance, defects in intestinal Na+-dependent glucose absorption cause glucose-galactose malabsorption with severe diarrhea and dehydration[4]. Compared with SGLT2, SGLT1 is mainly linked to intestinal absorption and later proximal-tubule glucose recovery, whereas SGLT2 mediates bulk renal glucose reabsorption in early proximal tubule segments[5]. For experimental applications, SGLT1 inhibition lowers and delays post-carbohydrate glucose excursion and can augment GLP-1 and PYY secretion, making SGLT1 inhibitors useful probes for intestinal glucose transport and enteroendocrine responses[1]. Structural studies of human SGLT1 with LX2761 provide a framework for studying inhibitor binding and transporter pharmacology[2].
References:
- [1]. Lehmann A, et al. Intestinal SGLT1 in metabolic health and disease. Am J Physiol Gastrointest Liver Physiol. 2016 Jun 1;310(11):G887-98. [Content Brief]
- [2]. Niu Y, et al. Structural mechanism of SGLT1 inhibitors. Nat Commun. 2022 Oct 28;13(1):6440. [Content Brief]
- [3]. Gorboulev V, et al. Na(+)-D-glucose cotransporter SGLT1 is pivotal for intestinal glucose absorption and glucose-dependent incretin secretion. Diabetes. 2012 Jan;61(1):187-96. [Content Brief]
- [4]. Turk E, et al. Glucose/galactose malabsorption caused by a defect in the Na+/glucose cotransporter. Nature. 1991 Mar 28;350(6316):354-6. [Content Brief]
- [5]. Ghezzi C, et al. Physiology of renal glucose handling via SGLT1, SGLT2 and GLUT2. Diabetologia. 2018 Oct;61(10):2087-2097. [Content Brief]
All Product Categories
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SGLT1 Related Products (32)
Related Products (32)
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SAR-7226
0 ImagesCat. No.: HY-150322CAS No.: 702638-25-3
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Janagliflozin
0 ImagesCat. No.: HY-178734CAS No.: 1800115-22-3Janagliflozin is orally active and highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor (IC50=0.0058 μM for SGLT2 and 4.802 μM for SGLT1). Janagliflozin inhibits SGLT2 in the proximal renal tubules, reducing glucose reabsorption and promoting urinary glucose excretion (UGE) to lower blood glucose levels. Janagliflozin is promising for research of type 2 diabetes mellitus.
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TA-1887
0 ImagesCat. No.: HY-12608CAS No.: 1003005-29-5Synonyms: JNJ-39933673TA-1887 (JNJ-39933673) is a highly potent, selective and orally active SGLT2 inhibitor (IC50: 1.4 nM) with antihyperglycemic effects. TA-1887 can be used in the research of diabetes.
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Trilobatin (Standard)
0 ImagesTrilobatin (Standard) is the analytical standard of Trilobatin. This product is intended for research and analytical applications. Trilobatin, a natural sweetener derived from?Lithocarpus polystachyus?Rehd, Trilobatin?is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
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SGLT2-IN-5
0 ImagesCat. No.: HY-180527SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes.
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SGLT2-IN-6
0 ImagesCat. No.: HY-180528SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes.
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Bexagliflozin diproline
0 ImagesCat. No.: HY-17604ACAS No.: 1118567-48-8Synonyms: EGT1442 diproline; EGT0001442 diproline; THR-1442 diprolineBexagliflozin diproline (EGT1442 diproline; EGT0001442 diproline; THR-1442 diproline) 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 diproline selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin diproline induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin diproline reduces blood glucose and HbA1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin diproline can be used for the research of type 2 diabetes mellitus, hypertensive stroke.
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Phlorizin (Standard)
0 ImagesPhlorizin (Floridzin) (Standard) is the analytical standard of Phlorizin. This product is intended for research and analytical applications. Phlorizin 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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TP0438836
0 ImagesCat. No.: HY-124664CAS No.: 957772-01-9TP0438836 (compound 30b) is a SGLT1 inhibitor, with IC50 values of 28 nM and 7 nM for hSGLT1 and hSGLT2, respectively. TP0438836 can be used in diabetes research.
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Sergliflozin-A
0 ImagesCat. No.: HY-165438CAS No.: 360775-96-8Sergliflozin-A is a compound used to inhibit type 2 diabetes. It can inhibit glucose transporters in the kidney, competitively inhibit hSGLT1 and hSGLT2, and mutations at different sites have different effects on its inhibitory effect.
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galacto-Dapagliflozin
0 ImagesCat. No.: HY-137145CAS No.: 1408245-02-2Galacto-dapagliflozin is a selective inhibitor for hSGLT2 with Ki of 25 nM.
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