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Dapagliflozin (BMS-512148) is a novel selective inhibitor of sodium-glucose co-transporter type 2. Sodium-glucose cotransporter-2 (SGLT2) inhibitors are a novel class of glucuretic, antihyperglycemic drugs that target the process of renal glucose reabsorption and induce glucuresis independently of insulin secretion or action. Dapagliflozin (BMS-512148) inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. In initial clinical trials, Dapagliflozin 10 mg reduced HbA1c by -0.54% (weighted mean differences (WMD), 95% CI -0.67 to -0.40) compared to placebo. Phase II and III clinical trials have demonstrated that dapagliflozin is a safe and effective method for treating type 2 diabetes. Dapagliflozin (BMS-512148) produces a sustained, dose-dependent reduction in plasma glucose levels while simultaneously improving insulin secretion and sensitivity. Therapy with dapagliflozin also results in a mild osmotic-diuretic effect that may account for decreases in total body weight (~2-3 kg) and blood pressure (systolic 2-5 mm Hg, diastolic 1.5-3 mm Hg), and increases in hematocrit (1-2%).
Patent. CN120624550A 2025 Sep 12; .
Patent. CN120624550A
Dapagliflozin purchased from AbMole
Patent. CN120983424A 2025 Nov 21; .
Patent. CN120983424A
Dapagliflozin purchased from AbMole
Exp Neurol. 2023 May 19;366:114448.
Dapagliflozin inhibits the activity of lateral habenula to alleviate diabetes mellitus-induced depressive-like behavior
Dapagliflozin purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | CHO cells |
| Preparation method | SGLT Binding Assays. Chinese hamster ovary (CHO) cells stably expressing human SGLT2 (hSGLT2) and human SGLT1 (hSGLT1) (Genbank accession numbers M95549 and M24847, respectively) were utilized for the development of transport assays using the selective SGLT substrate -methyl-D-glucopyranoside (AMG). Inhibitors were assayed for the ability to inhibit [14C]AMG uptake in a protein-free buffer over a 2 h incubation period. The response curve was fitted to an empirical four-parameter model to determine the inhibitor concentration at half maximal response, reported as EC50. Protein-free buffer was used to simulate the low-protein conditions of the glomerular filtrate, which bathes the SGLT targets on the lumenal surface of the proximal tubule in the kidney. |
| Concentrations | |
| Incubation time | 2 h |
| Animal Experiment | |
|---|---|
| Animal models | Normal Sprague Dawley rats |
| Formulation | 5% mpyrol, 20% PEG 400, and 20 mM sodium diphosphate |
| Dosages | single dose of 0.01-10 mg/kg |
| Administration | orally |
| Molecular Weight | 408.87 |
| Formula | C21H25ClO6 |
| CAS Number | 461432-26-8 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage | -20°C, dry, sealed |
| Related SGLT Products |
|---|
| Canagliflozin
Canagliflozin is a potent, selective sodium glucose co-transporter 2 inhibitor. |
| Empagliflozin
Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. |
| Phloridzin
Phloridzin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na+/K+-ATPase inhibitor. |
| Phloretin
Phloretin (NSC 407292; RJC 02792) is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). |
| Sotagliflozin
Sotagliflozin (LX-4211) is an orally active, first-in-class dual SGLT1/2 inhibitor with IC50s of 36 nM and 1.8 nM, respectively, and is used in studies related to type 1 diabetes and heart failure. |
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