| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
Dapagliflozin (formerly known as BMS-512148; trade names Farxiga in the US and Forxiga in the EU) is a potent and selective hSGLT2 (sodium-glucose transport proteins) inhibitor with anti-diabetic activity. It inhibits hSGLT2 with an EC50 of 1.1 nM, and exhibits1200-fold selectivity over hSGLT1. The FDA approved dapagliflozin in 2012 to treat type 2 diabetes. Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2) which are responsible for at least 90% of the glucose reabsorption in the kidney. Urine is the means by which blood glucose is expelled when this transporter mechanism is blocked.
| Targets |
hSGLT2 ( EC50 = 1.1 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The selective SGLT substrate α-methyl-D-glucopyranoside (AMG) is used in the development of transport assays using Chinese hamster ovary (CHO) cells that stably express human SGLT2 (hSGLT2) and human SGLT1 (\hSGLT1). The ability of dapagliflozin to inhibit [14C]AMG uptake is measured over the course of two hours of incubation in a protein-free buffer. The inhibitor concentration at half maximal response, or EC50, is found by fitting the response curve to an empirical four-parameter model. The low-protein environment of the glomerular filtrate, which covers the SGLT targets on the kidney's proximal tubule lumenal surface, is replicated using protein-free buffer.
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| Cell Assay |
Cells are collected for the cell survival assay following a 24-hour incubation period with either vehicle or dapagliflozin pretreatment in a 30-minute ischemia period. Any remaining cells are then counted using Trypan blue staining. The relative viable number of treated cells divided by the viable number of untreated cells is quantized to get the percentage survival.
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| Animal Protocol |
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| References |
| Molecular Formula |
C21H25CLO6
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|---|---|
| Molecular Weight |
408.87
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| Exact Mass |
408.13
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| Elemental Analysis |
C, 61.69; H, 6.16; Cl, 8.67; O, 23.48
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| CAS # |
461432-26-8
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| Related CAS # |
Dapagliflozin ((2S)-1,2-propanediol, hydrate); 960404-48-2; Dapagliflozin-d5; 1204219-80-6
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| Appearance |
White solid powder
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| SMILES |
CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)Cl
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| InChi Key |
JVHXJTBJCFBINQ-ADAARDCZSA-N
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| InChi Code |
InChI=1S/C21H25ClO6/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(24)17(11-23)28-21/h3-8,10,17-21,23-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1
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| Chemical Name |
(2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
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| Synonyms |
Dapagliflozin; BMS 512148; BMS512148; BMS-512148; trade name Farxiga in the US and Forxiga in the EU
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: ≥ 0.5 mg/mL (1.22 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 7: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30 mg/mL Solubility in Formulation 8: 33.33 mg/mL (81.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4458 mL | 12.2288 mL | 24.4577 mL | |
| 5 mM | 0.4892 mL | 2.4458 mL | 4.8915 mL | |
| 10 mM | 0.2446 mL | 1.2229 mL | 2.4458 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02981966 | Active Recruiting |
Drug: Dapagliflozin Drug: Placebo |
Diabetes Mellitus, Type 2 | The University of Texas Health Science Center at San Antonio |
May 23, 2019 | Phase 4 |
| NCT01714011 | Active Recruiting |
Drug: Dapagliflozin 10mg Tab Drug: Placebo |
Chronic Kidney Diseases Bone Diseases, Metabolic |
Mansoura University | November 10, 2022 | Phase 4 |
| NCT03199053 | Active Recruiting |
Drug: Dapagliflozin Drug: Saxagliptin |
Diabetes Mellitus, Type 2 | AstraZeneca | October 11, 2017 | Phase 3 |
| NCT04333823 | Active Recruiting |
Drug: Dapagliflozin 5mg Drug: Placebo |
Diabetes Mellitus, Type 1 | The Hospital for Sick Children | December 11, 2020 | Phase 3 |
| NCT03499704 | Active Recruiting |
Drug: Dapagliflozin Drug: Metformin |
Diabetes Mellitus, Type 2 | Celltrion Pharm, Inc. | February 11, 2020 | Phase 4 |
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