SGLT1 Inhibitor

Phloretin (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.

Phlorizin (Floridzin) is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i 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.

Sotagliflozin (LX-4211) is a potent dual SGLT2/1 inhibitor. Antidiabetic agents.

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.

Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a K_i of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

Bexagliflozin (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 HbA_1c 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.

Demethyl-LX2761 is a selective sodium-glucose cotransporter 1 (SGLT1) inhibitor. Demethyl-LX2761 can be used for the research of type 2 diabetes.

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.

Luseogliflozin (TS 071) is a potent, selective, orally active sodium-dependent glucose cotransporter (SGLT) 2 inhibitor, with an IC₅₀ of 2.26 nM, about 1765-fold selectivity over SGLT1 (IC₅₀, 3990 nM). Luseogliflozin has the protential for researching type 2 diabetes.

Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity sodium glucose cotransporter (SGLT2) inhibitor with K_i values of 1.95 μM, 2.14 μM, 43.1 μM, 8.57 μM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate is a proagent based on benzylpyrazole glucoside and is metabolized to its active form, Remogliflozin, in the body. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.

Phloretin (Standard) is the analytical standard of Phloretin. This product is intended for research and analytical applications. Phloretin (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.

Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin dihydrate promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin dihydrate reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin dihydrate induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin dihydrate also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.

T-1095 is a selective and orally active Na⁺-glucose cotransporter (SGLT) inhibitor with IC₅₀s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research.

SGLT1/2-IN-1 is a dual SGLT1/SGLT2 inhibitor extract from WO2015032272A1, compound 2 .

rel-Licogliflozin is a relative configuration of Licogliflozin (HY-109092). Licogliflozin is a sodium glucose cotransporter (SGLT1 and SGLT2) inhibitor.

SGLT1/2-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.

LX2761 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 is a SGLT1 and SGLT2 dual inhibitor. SAR-7226 can be used for research of type 2 diabetes.

Janagliflozin 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.