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
-
SGLT2 Related Products (67)
Related Products (67)
-
rel-Licogliflozin
0 ImagesCat. No.: HY-109092ACAS No.: 2730989-98-5Synonyms: rel-LIK066rel-Licogliflozin is a relative configuration of Licogliflozin (HY-109092). Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.
-
Atigliflozin
0 ImagesCat. No.: HY-14810CAS No.: 647834-15-9Synonyms: AVE-2268Atigliflozin (AVE-2268) is an orally active and selective SGLT-2 inhibitor, with IC50s of 10 nM and 8.2 μM for hSGLT-2 and hSGLT-1) respectively. Atigliflozin can lower the blood glucose and improve the impaired oral glucose tolerance. Atigliflozin can be used for research of type II diabetes mellitus.
-
WAY-123783
0 ImagesCat. No.: HY-114598CAS No.: 152595-59-0WAY-123783 is a potent, selective and orally active sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor producing activity after metabolism. WAY-123783 can increase the excretion of sugar in urine and at the same time lower the blood sugar level in db/db mice (ED50 = 9.85 mg/kg). WAY-123783 can be used for the research of metabolic disease, such as diabetes.
-
SGLT1/2-IN-8
0 ImagesCat. No.: HY-169821CAS No.: 2206679-16-3SGLT1/2-IN-8 (compound 8) is a potent and orally active SGLT1/2 dual inhibitor with IC50 values of 4 nM and 1 nM, respectively. SGLT1/2-IN-8 exhibits anti-hyperglycemic effects and can be utilized in relevant research.
-
YM-543
0 ImagesCat. No.: HY-125327CAS No.: 1610007-47-0YM-543 is a selective SGLT2 inhibitor that effectively reduces hyperglycemia in type 2 diabetic mice through increased urinary glucose excretion. YM-543 demonstrates potent inhibition of both mouse and human SGLT2 activities at nanomolar concentrations. YM-543, when administered orally, significantly improves glucose tolerance in diabetic models and sustains its effects for over 12 hours. YM-543, in combination with other antidiabetic agents like rosiglitazone or metformin, enhances the therapeutic effects on diabetic symptoms. YM-543 does not affect blood glucose levels in normal mice, indicating its specificity for diabetic conditions.
-
LX2761
0 ImagesLX2761 is an orally active, dual SGLT1/SGLT2 inhibitor with IC50 values of 2.2 nM and 2.7 nM against human SGLT1 and SGLT2, respectively. LX2761 locks human SGLT1 in an outward-open conformation and blocks its putative water permeation pathway. After oral administration, LX2761 is confined exclusively to the intestinal lumen, delays intestinal glucose absorption, regulates intestinal glucose metabolism, increases cecal glucose levels, reduces cecal pH, improves glycemic control and elevates plasma total GLP-1 levels. However, LX2761 induces diarrhea in a dose-dependent manner. LX2761 can be used in diabetes-related research.
-
SAR-7226
0 ImagesCat. No.: HY-150322CAS No.: 702638-25-3
-
Pragliflozin-13C6
0 ImagesCat. No.: HY-14894S2CAS No.: 2743031-48-1Synonyms: ASP1941-13C6Pragliflozin-13C6 (ASP1941-13C6) is 13C labeled Ipragliflozin. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.
-
Velagliflozin proline hydrate
0 ImagesVelagliflozin proline hydrate is the clinical form of Velagliflozin (HY-109018). Velagliflozin is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor with antidiabetic activity. Velagliflozin reduces renal glucose reabsorption and stimulates glycosuria, which lowers blood sugar and insulin concentrations.
-
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.
-
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.
-
SGLT2-IN-3
0 ImagesCat. No.: HY-178167SGLT2-IN-3 is a sodium-glucose co-transporter 2 (SGLT2) inhibitor. SGLT2-IN-3 can inhibit glucose uptake. SGLT2-IN-3 can be used for the research of metabolic disease, such as diabetes.
-
YM543 free base
0 ImagesCat. No.: HY-122613CAS No.: 655237-16-4YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes.
-
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.
-
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.
-
Canagliflozin (Standard)
0 ImagesSynonyms: JNJ 28431754 (Standard)Canagliflozin (Standard) is the analytical standard of Canagliflozin. This product is intended for research and analytical applications. Canagliflozin (JNJ 28431754) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.
-
Ipragliflozin (Standard)
0 ImagesSynonyms: ASP1941 (Standard)Ipragliflozin (Standard) is the analytical standard of Ipragliflozin. This product is intended for research and analytical applications. Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC50s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.
-
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.
-
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.
