Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin induces HIF1 expression and attenuates renal IR injury.
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Dapagliflozin Estructura química
No. CAS : 461432-26-8
This product is a controlled substance and not for sale in your territory.
Dapagliflozin purchased from MedChemExpress. Usage Cited in:
Life Sci. 2023 Apr 4;121671.
[Abstract]
Dapagliflozin (DAPA; 10 μM; 24 hours) significantly decreases the expression of YAP/TAZ and increases the ratios of p-YAP/YAP and pTAZ/TAZ under high glucose conditions in HK-2 cells.
Dapagliflozin purchased from MedChemExpress. Usage Cited in:
Life Sci. 2023 Apr 4;121671.
[Abstract]
Dapagliflozin (DAPA; 10, 20 μM; 24 h) significantly reverses the decrease in cell viability caused by high glucose in HK-2 cells.
Dapagliflozin purchased from MedChemExpress. Usage Cited in:
Life Sci. 2023 Apr 4;121671.
[Abstract]
Dapagliflozin (DAPA; 10 μM; 24 hours) significantly reduces the high glucose-induced increase in YAP/TAZ expression in HK-2 cells.
The expression of IRS1 significantly decreases. The phosphorylation levels of Akt1, Akt2, and S6 are significantly reduced in livers of db/db mice.
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Descripciòn
Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine[1]. Dapagliflozin induces HIF1 expression and attenuates renal IR injury[2].
IC50 & Target
SGLT2
In Vitro
Dapagliflozin (0-10 μM；24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner[2].Dapagliflozin (0-10 μM；2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells[2]..
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Dapagliflozin Related Antibodies
Cell Viability Assay[1]
Cell Line:
Hypoxic HK2 cells
Concentration:
0 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time:
24 hours
Result:
Improved the cell viability in a dose-dependent manner compared with control cells.
Western Blot Analysis[1]
Cell Line:
Hypoxic HK2 cells, Normoxic HK2 cells
Concentration:
0 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time:
24 hours
Result:
Induced HIF1 expression in hypoxic and normoxic HK2 cells.
In Vivo
Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DMSO : ≥ 100 mg/mL (244.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 50 mg/mL (122.29 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (81.52 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
[1]. Pelissier T, et al. The orofacial capsaicin test in rats: effects of different capsaicin concentrations and morphine. Pain. 2002 Mar;96(1-2):81-7.
[Content Brief]
[1]. Pelissier T, et al. The orofacial capsaicin test in rats: effects of different capsaicin concentrations and morphine. Pain. 2002 Mar;96(1-2):81-7.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
H2O / DMSO
1 mM
2.4458 mL
12.2288 mL
24.4577 mL
61.1441 mL
5 mM
0.4892 mL
2.4458 mL
4.8915 mL
12.2288 mL
10 mM
0.2446 mL
1.2229 mL
2.4458 mL
6.1144 mL
15 mM
0.1631 mL
0.8153 mL
1.6305 mL
4.0763 mL
20 mM
0.1223 mL
0.6114 mL
1.2229 mL
3.0572 mL
25 mM
0.0978 mL
0.4892 mL
0.9783 mL
2.4458 mL
30 mM
0.0815 mL
0.4076 mL
0.8153 mL
2.0381 mL
40 mM
0.0611 mL
0.3057 mL
0.6114 mL
1.5286 mL
50 mM
0.0489 mL
0.2446 mL
0.4892 mL
1.2229 mL
60 mM
0.0408 mL
0.2038 mL
0.4076 mL
1.0191 mL
80 mM
0.0306 mL
0.1529 mL
0.3057 mL
0.7643 mL
100 mM
0.0245 mL
0.1223 mL
0.2446 mL
0.6114 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Dapagliflozin Related Classifications
Membrane Transporter/Ion Channel
SGLT
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