For research use only.
Catalog No.S1548 Synonyms: BMS-512148
CAS No. 461432-26-8
Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Selleck's Dapagliflozin has been cited by 18 publications
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Effects of once-daily administration of DAPA, DAPA switched to (DAla2)GIP or saline vehicle on (AeD) DEXA images, (E) body fat, (F) lean mass, (G) bone mineral content and (H) bone mineral density in high fat fed mice. Mice received saline vehicle (0.9% wt/vol; po), DAPA (1 mg/kg; po) once-daily over 28 days, or DAPA (1 mg/kg; po) once-daily over 14 days followed by (DAla2)GIP (25 nmol/kg; ip) once-daily for 14 days. Lean control mice received saline vehicle once-daily. White bars=lean controls; grey bars=HF controls; black bars=DAPA; and hatched bars=DAPA / GIP. Values are mean ± SEM for groups of 6-8 mice. *p < 0.05 and **p < 0.01 compared to HF controls.
Mol Cell Endocrinol, 2016, 420:37-45.. Dapagliflozin purchased from Selleck.
Effects of Dapagliflozin at different concentrations on the amplitude of shortening in ventricular myocytes from Streptozotocin-induced diabetic and Control rats. Graph showing the mean amplitudes (AMP) of shortening, expressed as a percentage of shortening in STZ and Control myocytes superfused with normal Tyrode(NT) and in the presence of different concentrations of DAPA. Data are mean+S.E.M. (n = 182 cells from 30 rats). Horizontal lines above the bars represent significant differences at the level of P<0.05.
Mol Cell Biochem,2015, 400(1-2):57-68.. Dapagliflozin purchased from Selleck.
Percentage of viable hCPCs following treatment with dapagliflozin and 25 mM d-glucose for 72 h. Viability was not significant different in hCPCs exposed to 1 μM dapagliflozin and 25 mM d-glucose for 72 h and in the control. Results are presented as means ± SD. *p<0.05 vs. control. **p<0.01 vs. control.
Biomol Ther, 2016, 24(4):363-70. Dapagliflozin purchased from Selleck.
Purity & Quality Control
Choose Selective SGLT Inhibitors
|Description||Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.|
|Features||More potent stimulator of glucosuria than other SGLT2 inhibitors.|
Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50.  Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly selective versus GLUT transporters and displays 8–9% inhibition in protein-free buffer at 20 μM and virtually no inhibition in the presence of 4% bovine serum albumin.  Dapagliflozin has good permeability across Caco-2 cell membranes and is a substrate for P-glycoprotein (P-gp) but not a significant P-gp inhibitor. Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM. Dapagliflozin shows no inhibitory responses or induction to human P450 enzymes. The in vitro metabolic pathways Dapagliflozin are glucuronidation, hydroxylation, and O-deethylation. 
|In vivo||Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the metabolic stability conferred by the C-glucoside linkage. Dapagliflozin displays a favorable absorption, distribution, metabolism, and excretion (ADME) profile and is orally bioavailable.  Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and increase in urine volume in normal rats over 24 hours post-dose. Dapagliflozin induces increase in urine glucose and urine volume excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats. Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2 weeks of treatment, without any marker of renal or liver toxicity.  Dapagliflozin significantly reduces the development of hyperglycaemia, with lowered blood glucose. Dapagliflozin could improve the insulin sensitivity, reduce β-cell mass and the development of impaired pancreatic function. |
|In vitro||DMSO||82 mg/mL (200.55 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG300+5% tween80+50% H2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04445714||Not yet recruiting||Drug: dapagliflozin and saxagliptin||Type 2 Diabetes Mellitus||AstraZeneca||June 30 2020||Phase 4|
|NCT04035031||Recruiting||Drug: Forxiga 10mg|Drug: Placebo||Diabetes Mellitus Type 1||University Hospital Inselspital Berne||January 9 2020||Phase 3|
|NCT04080518||Recruiting||Drug: Dapagliflozin 10 MG [Farxiga]||Diabetes Mellitus|Heart Failure||National Heart Centre Singapore|Duke-NUS Medical School (Singapore)||November 11 2019||Phase 4|
|NCT04120623||Not yet recruiting||Drug: Dapagliflozin 10 MG|Drug: Insulin Aspart||Type 2 Diabetes Mellitus||Nanjing First Hospital Nanjing Medical University||October 1 2019||Phase 4|
|NCT04090580||Recruiting||Diagnostic Test: Continuous glucose monitoring||Type 2 Diabetes||Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|AztraZeneca||August 27 2019||Phase 4|
|NCT03624803||Completed||--||Type-2 Diabetes||AstraZeneca||March 9 2019||--|
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