Catalog No.S1548 Synonyms: BMS-512148
Molecular Weight(MW): 408.87
Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Cited by 7 Publications
4 Customer Reviews
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.
(B) Clonogenic survival of prostate cancer cells treated with Canagliflozin, Dapagliflozin or Salicylate and expressed relative to the vehicle controls.
Mol Metab, 2016, 5(10):1048-56.. 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 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)|
|Ethanol||17 mg/mL (41.57 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|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|
|NCT04035031||Not yet recruiting||Drug: Forxiga 10mg|Drug: Placebo||Diabetes Mellitus Type 1||University Hospital Inselspital Berne||September 1 2019||Phase 3|
|NCT04080518||Recruiting||Drug: Dapagliflozin 10 MG [Farxiga]||Diabetes Mellitus|Heart Failure||National Heart Centre Singapore|Duke-NUS Medical School (Singapore)||September 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||Recruiting||--||Type-2 Diabetes||AstraZeneca||March 9 2019||--|
|NCT04084184||Completed||Drug: HGP1812|Drug: HGP1602||Healthy||Hanmi Pharmaceutical Company Limited||March 15 2019||Phase 1|
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