sglt2

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1/4/5/6. Empagliflozin is used for the treatment of type 2 diabetes.

Licogliflozin (LIK066) is an inhibitor of sodium-glucose cotransporter (SGLT1 and SGLT2).

Sergliflozin A is a selective SGLT2 inhibitor that induces diabetes in a dose-dependent manner. It reduces hyperglycemia.

Ipragliflozin (ASP1941) is under investigation in Type 2 Diabetes and Diabetes Mellitus, Type 2.

Phloretin (NSC-407292) is a well-known inhibitor of eukaryotic urea transporters, blocks VacA-mediated urea and ion transport. Phloretin is a dihydrochalcone, a type of natural phenols. It can be found in apple tree leaves and the Manchurian apricot. It promotes potent antioxidative activities in peroxynitrite scavenging and the inhibition of lipid peroxidation. It has been found to inhibit the growth of several cancer cells and induce apoptosis of B16 melanoma and HL60 human leukemia cells.

Sotagliflozin (LX-4211, LP-802034) is an oral dual inhibitor of sodium-glucose cotransporter 1/2 (SGLT1/SGLT2) (SGLT2, IC₅₀ ≈ 1.8 nM; SGLT1, IC₅₀ ≈ 36 nM) used as an antidiabetic agent. Sotagliflozin is used in research on cardiovascular disease and diabetes.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

Ipragliflozin is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.

HSK0935 is a highly selective and orally available SGLT2 inhibitor (IC50: 1.3 nM). It has antihyperglycemic activities.

Velagliflozin is an orally available inhibitor of sodium-glucose cotransporter 2.

Canagliflozin hemihydrate (TA 7284) is a drug of the gliflozin class or subtype 2 sodium-glucose transport inhibitors used for the treatment of type 2 diabetes. SGLT2 is responsible for at least 90% of renal glucose reabsorption (SGLT1 being responsible for the remaining 10%). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories.

Sergliflozin etabonate (KGT-1251) is an inhibitor of SGLT2 and can be used in studies about type 2 diabetes and obesity.

Remogliflozin etabonate (GSK189075A) is a prodrug of regaliflozin and an inhibitor SGLT2 with Ki values of 1.95, 2.14, 8.57, and 43.1μM for hSGLT2, rSGLT2, rSGLT1, and hSGLT1, respectively.

Enavogliflozin (DWP-16001) is an orally available small molecule and sodium glucose transporter 2 inhibitor.

PF-04971729 (Ertugliflozin (PF-04971729)) is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2).

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific inhibitor of SGLT2, 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, respectively.

O-Desethyl Dapagliflozin (Empagliflozin-4) is a SGLT2 inhibitor, IC50=33nM.

Bexagliflozin (EGT1442) is a potent, selective sodium glucose co-transporter 2 (SGLT2) inhibitor with IC50 values of 2 nM for human SGLT2 and 5.6 μM for human SGLT1.

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).

Kushenol C is a good 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenger, and it exhibits inhibitory activity against Sodium-dependent glucose cotransporter 2(SGLT2). Kushenol C shows antimicrobial activity against Staphylococcus aureus and Streptococcus mutan

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a selective and orally active hSGLT2 inhibitor with an IC50 of 0.877 nM, suitable for studies on the treatment of type 2 diabetes mellitus.

SGLT2-IN-2 (Compound E9) is an inhibitor of SGLT2 and significantly enhances the inhibition of SGLT2, NHE1, and SOD enzyme activities. It provides protection against myocardial cell damage induced by glucose-free DMEM. Additionally, SGLT2-IN-2 markedly improves cardiac function in TAC-induced heart failure (HF) mice, suppressing myocardial cell hypertrophy and collagen deposition. It reduces myocardial tissue damage and boosts autophagy in damaged myocardial cells, increasing the survival rate of HF mice.

SGLT2-IN-3 is an inhibitor of sodium-glucose cotransporter 2 (SGLT2), capable of suppressing glucose uptake. It is applicable for research into metabolic disorders, such as diabetes.

SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values of 0.8 nM for SGLT2, 23 nM for SGLT1, and 58 nM for DPP4. In diabetic rat models, SGLT2-IN-5 effectively regulates blood glucose and increases the levels of active GLP-1. It is suitable for research on type 2 diabetes.