| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
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| Other Sizes |
Dapagliflozin impurity is an isomer of Dapagliflozin which is a SGLT2 (sodium-glucose transporter 2) inhibitor approved in 2012 for the treatment of type 2 diabetes.
| Targets |
Isomer and metabolite of Dapagliflozin
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|---|---|
| References | |
| Additional Infomation |
Objective: Dapagliflozin increases urinary glucose excretion by selectively inhibiting renal sodium-glucose cotransporter 2 (SGLT2), and its mechanism of action is insulin-independent, potentially complementary to the mechanisms of action of other oral hypoglycemic agents. This study aimed to evaluate the potential pharmacokinetic (PK) interactions between dapagliflozin and pioglitazone, metformin, glimepiride, or sitagliptin in healthy subjects after a single dose. Methods: In an open-label, randomized, three-period, three-group crossover study, 24 subjects received 50 mg dapagliflozin, 45 mg pioglitazone, or a combination of both, while 18 subjects received 20 mg dapagliflozin, 1000 mg metformin, or a combination of both. In an open-label, randomized, five-period, five-treatment-regimen unbalanced crossover study, 18 subjects initially received 20 mg dapagliflozin, 4 mg glimepiride, or a combination of both, followed by 100 mg sitagliptin or sitagliptin combined with 20 mg dapagliflozin. Blood samples were collected continuously for 72 hours during each treatment cycle. The absence of pharmacokinetic interactions was defined as a geometric mean ratio of combination therapy to monotherapy and its 90% confidence interval (CI) within the range of 0.80–1.25. Results: Combination therapy of dapagliflozin with pioglitazone, metformin, glimepiride, or sitagliptin had no effect on the peak plasma concentration (Cmax) or area under the plasma concentration-time curve (AUC) of dapagliflozin. Similarly, dapagliflozin did not affect the Cmax or AUC of the concomitant drugs, only slightly expanding the 90% confidence interval of the geometric mean ratio of glimepiride's AUC (upper limit 1.29) and the 90% confidence interval of the geometric mean ratio of pioglitazone's Cmax (lower limit 0.75). All monotherapy and combination therapies were well tolerated. Conclusion: Dapagliflozin can be used in combination with pioglitazone, metformin, glimepiride, or sitagliptin without dose adjustment of any of these drugs. [1]
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| Molecular Formula |
C21H25CLO7
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|---|---|
| Molecular Weight |
424.872006177902
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| Exact Mass |
424.128
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| CAS # |
960404-86-8
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| PubChem CID |
59648701
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
|
| Heavy Atom Count |
29
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| Complexity |
515
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| Defined Atom Stereocenter Count |
5
|
| SMILES |
O[C@@]1([C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1)C1C=CC(Cl)=C(CC2C=CC(OCC)=CC=2)C=1
|
| InChi Key |
KYDGWGYAUCJZDV-ADAARDCZSA-N
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| InChi Code |
InChI=1S/C21H25ClO7/c1-2-28-15-6-3-12(4-7-15)9-13-10-14(5-8-16(13)22)21(27)20(26)19(25)18(24)17(11-23)29-21/h3-8,10,17-20,23-27H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1
|
| Chemical Name |
(2S,3R,4S,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-2,3,4,5-tetrol
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| Synonyms |
Dapagliflozin impurity; 960404-86-8; Dapagliflozin Impurity 10; Dapagliflozin hydroxy impurity; Hydroxy dapagliflozin; 2GLW9C3QQ3; (2S,3R,4S,5S,6R)-2-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol; (2S,3R,4S,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-2,3,4,5-tetrol;
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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) |
DMSO : ~25 mg/mL (~58.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (3.37 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.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (3.37 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 14.3 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3537 mL | 11.7683 mL | 23.5366 mL | |
| 5 mM | 0.4707 mL | 2.3537 mL | 4.7073 mL | |
| 10 mM | 0.2354 mL | 1.1768 mL | 2.3537 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.
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