SGLT Inhibitor

Tofogliflozin hydrate (CSG-452 hydrate) is a potent and highly specific sodium/glucose cotransporter 2 (SGLT2) inhibitor with an IC₅₀ of 2.9 nM and K_i 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.

Ipragliflozin (L-Proline) 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.

Empagliflozin-d₄ is deuterium labeled Empagliflozin. Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC₅₀ of 3.1 nM for human SGLT-2.

Ertugliflozin 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.

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.

Velagliflozin is an orally available sodium-glucose cotransporter 2 (SGLT2) inhibitor, with anti-diabetic activity.

Dapagliflozin-d₅ is a deuterium labeled Dapagliflozin (HY-10450). Dapagliflozin is a competitive SGLT2 inhibitor.

Tianagliflozin is a sodium/glucose cotransporter 2 (SGLT-2) inhibitor with potential for investigation in 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.

Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.

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.

SGLT2-IN-2 (Compound E9) is an inhibitor of SGLT2. SGLT2-IN-2 significantly enhances the inhibition of SGLT2, NHE1, and SOD enzyme activity. SGLT2-IN-2 has protective effect on the glucose-free DMEM-induced injured cardiomyocytes. SGLT2-IN-2 significantly improves cardiac function in TAC-induced HF mice and inhibits cardiomyocyte hypertrophy as well as collagen deposition. SGLT2-IN-2 can ameliorate myocardial tissue damage and enhance mitochondrial autophagy in injured cardiomyocytes, thereby increasing survival rates in HF mice.

Canagliflozin-d₄ (JNJ 28431754-d₄) is a deuterium labeled Canagliflozin. Canagliflozin is a selective SGLT2 inhibitor.

Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.

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.

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

Remogliflozin (Remogliflozin A) is an orally active, highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor, with a K_i of 12.4 nM for human SGLT2 and 26.0 nM for rat SGLT2. Remogliflozin increases urinary glucose excretion by inhibiting renal glucose reabsorption. Without insulin stimulation, remogliflozin suppresses the elevation of plasma glucose, reduces fasting blood glucose and glycated hemoglobin, and improves glycosuria, hyperglycemia, hyperinsulinemia, hypertriglyceridemia and insulin resistance in diabetic rodents. Remogliflozin can be used in research related to type 2 diabetes.

HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC₅₀ of 1.3 nM. Antihyperglycemic activities.

Sergliflozin etabonate (GW-869682X) is a potent and orally active sodium glucose cotransporter (SGLT2) inhibitor. Sergliflozin etabonate shows antidiabetic and antihyperglycemic effects. Sergliflozin etabonate significantly reduces non-fasting blood glucose levels in diabetic mice. Sergliflozin etabonate has the potential for the research of diabetes.