SGLT

BI-44847 is a selective and orally active inhibitor of the sodium-glucose cotransporter 2 (SGLT2), primarily targeting glucose reabsorption in the kidneys. This compound is known to enhance urinary glucose excretion (UGE) and reduce HbA1c levels, thus improving both fasting and postprandial glucose levels. BI-44847 is valuable for research applications focused on understanding and treating type 2 diabetes mellitus (T2DM).

YM-543 is a selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2), designed to reduce hyperglycemia in type 2 diabetes models. It exhibits potent inhibition of both human and mouse SGLT2 activities at nanomolar concentrations, ultimately increasing urinary glucose excretion and improving glucose tolerance. When administered orally, YM-543 maintains its therapeutic effects for over 12 hours and enhances the action of other antidiabetic agents, such as rosiglitazone or metformin, without affecting blood glucose levels in non-diabetic models. This specificity underscores its potential utility in diabetic research and therapeutic strategies.

SAR-7226 is a dual inhibitor of sodium-glucose co-transporters SGLT1 and SGLT2. It demonstrates significant biological activity in reducing glucose reabsorption in the kidneys and intestines, making it a valuable tool for studying the mechanisms underlying type 2 diabetes. This compound is useful for research aimed at understanding the pharmacological modulation of glucose homeostasis and developing therapeutic strategies for managing diabetes and related metabolic disorders.

Mizagliflozin (sebacate) is a selective inhibitor of sodium-glucose cotransporter 1 (SGLT1), demonstrating significant potential in enhancing vascular cognitive impairment associated with small vessel disease. By inhibiting SGLT1 activity in neurons, Mizagliflozin (sebacate) effectively improves cerebral blood flow and cognitive functions such as spatial learning and memory in relevant mouse models. Additionally, Mizagliflozin (sebacate) has been shown to increase the survival rate of IL-1β-treated PC12HS cells, supporting its role in neuroprotection. This compound is valuable for research into therapeutic strategies for cognitive deficits linked to vascular health.

Pragliflozin-13C6 is a stable isotope-labeled form of Ipragliflozin, a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor. This compound demonstrates inhibitory activity with IC50 values of 7.38 nM for human SGLT2 and significantly higher values for SGLT1, making it a potent antidiabetic agent. Pragliflozin-13C6 is primarily utilized in pharmacokinetic studies and metabolic experiments to trace the pathways and mechanisms of Ipragliflozin in biological systems.

Velagliflozin proline hydrate is an oral sodium-glucose cotransporter 2 (SGLT2) inhibitor that exhibits significant antidiabetic activity. By diminishing renal glucose reabsorption, Velagliflozin promotes glycosuria, effectively lowering blood glucose levels and insulin concentrations. This compound is primarily utilized in research focused on diabetes management and metabolic disorders.

Janagliflozin is a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2), exhibiting an IC50 of 0.0058 μM for SGLT2 and 4.802 μM for SGLT1. This compound functions primarily in the proximal renal tubules to inhibit glucose reabsorption, thereby enhancing urinary glucose excretion and lowering blood glucose levels. Janagliflozin holds potential for research applications targeting type 2 diabetes mellitus.

TA-1887 is a highly potent and selective SGLT2 inhibitor, exhibiting an IC50 of 1.4 nM. This compound demonstrates significant antihyperglycemic effects, making it valuable in the study of diabetes and glucose metabolism. Researchers can utilize TA-1887 to investigate the therapeutic potential and mechanisms of SGLT2 inhibition in metabolic disorders.

Dapagliflozin methyl acetate is a potent SGLT2 inhibitor, primarily targeting sodium-glucose co-transporter 2. It plays a crucial role in regulating glucose reabsorption in the kidneys, which is significant for managing blood glucose levels. This compound is commonly utilized in research related to type 2 diabetes and metabolic disorders, facilitating investigations into the pharmacological effects and potential therapeutic applications of SGLT2 inhibition.

YM543 free base is a potent, orally active inhibitor of the sodium-glucose cotransporter 2 (SGLT2). This compound effectively lowers blood glucose levels, making it a valuable tool in diabetes research. Its mechanism of action provides insights into glucose homeostasis and offers potential therapeutic strategies for managing diabetic conditions.

Ertugliflozin-d5 is a deuterium-labeled form of Ertugliflozin, a selective and potent inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2). With an IC50 of 0.877 nM against human SGLT2, it effectively reduces glucose reabsorption in the kidneys, making it relevant in research aimed at understanding type 2 diabetes mellitus treatment mechanisms. This stable isotope-labeled reagent is valuable for pharmacokinetic studies and metabolic tracing in biological systems.

Remogliflozin etabonate-d7 is the deuterium-labeled variant of Remogliflozin etabonate, a selective sodium glucose cotransporter 2 (SGLT2) inhibitor. With Ki values of 1.95 μM for hSGLT2 and 2.14 μM for rSGLT2, it demonstrates notable inhibition of glucose reabsorption in renal tissues. Remogliflozin etabonate is metabolized to its active form within the body, contributing to its antidiabetic effects observed in rodent models. This stable isotope-labeled compound is valuable for pharmacokinetic studies and metabolic research involving SGLT2 inhibition.

TP0438836 is a selective inhibitor of the sodium-glucose cotransporter 1 (SGLT1), demonstrating an IC50 value of 28 nM for human SGLT1 and 7 nM for human SGLT2. This compound is of significant interest in diabetes research, as it may help elucidate the role of glucose absorption in glucose homeostasis and insulin regulation. TP0438836 can be utilized in studies aimed at developing therapeutic strategies for managing diabetes and related metabolic disorders.

Sergliflozin-A is a selective inhibitor of sodium-glucose co-transporter proteins SGLT1 and SGLT2, which play key roles in glucose reabsorption in the kidney. By competitively inhibiting these transporters, Sergliflozin-A contributes to reduced glucose reabsorption, making it a valuable compound in the study and treatment of type 2 diabetes. Its efficacy may vary with different mutations in target sites, underscoring its potential for tailored therapeutic applications in metabolic disorders.

Galacto-Dapagliflozin is a selective inhibitor of the human sodium-glucose cotransporter 2 (hSGLT2), exhibiting a Ki value of 25 nM. This compound demonstrates significant potential in modulating glucose homeostasis and promoting renal glucose excretion. Its application extends to research in metabolic disorders, particularly in the study of type 2 diabetes and related glucose regulation mechanisms.

Fluoro-Dapagliflozin is a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor, exhibiting a Ki value of 5.3 nM for SGLT2 and 330 nM for SGLT1. It functions by blocking glucose transport, thereby reducing glucose absorption in the kidneys. This compound is valuable for research applications aimed at understanding glucose homeostasis, diabetic metabolism, and the therapeutic potential in managing type 2 diabetes.

Phlorizin dihydrate is a biochemical reagent that acts as a specific inhibitor of glucose transporters, primarily SGLT1 and SGLT2. Its key biological activity includes the inhibition of glucose reabsorption in the kidneys, making it valuable for studies in diabetes and renal physiology. Phlorizin dihydrate is commonly used in research applications involving glucose transport mechanisms and metabolic profiling.