Dapagliflozin

Catalog No.S1548 Batch:S154807

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Technical Data

Formula

C21H25ClO6
Molecular Weight 408.87 CAS No. 461432-26-8
Solubility (25°C)* In vitro DMSO 82 mg/mL (200.55 mM)
Ethanol 17 mg/mL (41.57 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Dapagliflozin is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Targets
hSGLT2 [1]
(CHO cells)
1.1 nM(EC50)
In vitro

Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. [1]

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. [2]

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. [3]
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. [1]

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. [2]

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. [4]
Features More potent stimulator of glucosuria than other SGLT2 inhibitors.

Protocol (from reference)

Kinase Assay:

[1]
  • SGLT Binding Assays

    Chinese hamster ovary (CHO) cells stably expressing human SGLT2 (hSGLT2) and human SGLT1 (\hSGLT1) are utilized for the development of transport assays using the selective SGLT substrate α-methyl-D-glucopyranoside (AMG). Dapagliflozin is assayed for the ability to inhibit [14C]AMG uptake in a protein- free buffer over a 2 hours incubation period. The response curve is fitted to an empirical four-parameter model to determine the inhibitor concentration at half maximal response, reported as EC50. Protein-free buffer is 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.
Animal Study:

[1]
  • Animal Models

    Normal Sprague Dawley rats or streptozotocin induced male Sprague Dawley rats

  • Dosages

    0.01-10 mg/kg (1 mL/kg) followed by a 50% glucose solution (2 g/kg)

  • Administration

    Dosed orally

References

  • https://pubmed.ncbi.nlm.nih.gov/18260618/
  • https://pubmed.ncbi.nlm.nih.gov/18356408/
  • https://pubmed.ncbi.nlm.nih.gov/19996149/
  • https://pubmed.ncbi.nlm.nih.gov/20880347/
  • https://pubmed.ncbi.nlm.nih.gov/34836340/

Customer Product Validation

<p>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.<br /> </p>

, , Mol Cell Endocrinol, 2016, 420:37-45.

<p>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.</p>

, , Mol Cell Biochem,2015, 400(1-2):57-68.

(B) Clonogenic survival of prostate cancer cells treated with Canagliflozin, Dapagliflozin or Salicylate and expressed relative to the vehicle controls.

Data from [ , , Mol Metab, 2016, 5(10):1048-56. ]

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.

Data from [ , , Biomol Ther, 2016, 24(4):363-70 ]

Selleck's Dapagliflozin has been cited by 47 publications

REDD1 expression in podocytes facilitates renal inflammation and pyroptosis in streptozotocin-induced diabetic nephropathy [ Cell Death Dis, 2025, 16(1):79] PubMed: 39920111
Low-dose metformin requires brain Rap1 for its antidiabetic action [ Sci Adv, 2025, 11(31):eadu3700] PubMed: 40737402
Single-nucleus RNA sequencing identifies cell-type-specific effects of sodium-glucose co-transporter 2 inhibitors in human myocardial slices [ Eur Heart J, 2024, 31:ehae472.] PubMed: 39082743
ALDH2 mediates the effects of sodium-glucose cotransporter 2 inhibitors (SGLT2i) on improving cardiac remodeling [ Cardiovasc Diabetol, 2024, 23(1):380] PubMed: 39462342
SGLT2i improves kidney senescence by down-regulating the expression of LTBP2 in SAMP8 mice [ J Cell Mol Med, 2024, 28(6):e18176] PubMed: 38454800
SGLT2i improves kidney senescence by down-regulating the expression of LTBP2 in SAMP8 mice [ J Cell Mol Med, 2024, 28(6):e18176] PubMed: 38454800
Dapagliflozin improves skeletal muscle insulin sensitivity through SIRT1 activation induced by nutrient deprivation state [ Sci Rep, 2024, 14(1):16878] PubMed: 39043740
SGLT2 inhibitors attenuate endothelial to mesenchymal transition and cardiac fibroblast activation [ Sci Rep, 2024, 14(1):16459] PubMed: 39013942
Dapagliflozin Mitigated Elevated Disomic and Diploid Sperm in a Mouse Model of Diabetes and Recover the Disrupted Ogg1, Parp1, and P53 Gene Expression [ Biomedicines, 2023, 10.3390/biomedicines11112980] PubMed: 38001980
Impacts of the DPP-4 Inhibitor Saxagliptin and SGLT-2 Inhibitor Dapagliflozin on the Gonads of Diabetic Mice [ Biomedicines, 2023, 11(10)2674] PubMed: 37893048

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