Dapagliflozin [461432-26-8]
Cat# HY-10450-5mg
Size : 5mg
Brand : MedChemExpress
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 Chemical Structure
CAS No. : 461432-26-8
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- 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 (DAPA; 10 μM; 24 hours) significantly reduces the high glucose-induced increase in YAP/TAZ expression in HK-2 cells.
- Dapagliflozin (DAPA; 10, 20 μM; 24 h) significantly reverses the decrease in cell viability caused by high glucose in HK-2 cells.
- Dapagliflozin increases the LC3-II to LC3-I expression ratio in the liver.
- Effects of Dapagliflozin and Empagliflozin on p62 expression in LPS-untreated and LPS-treated RAW264.7 cells.
- The expression of IRS1 significantly decreases. The phosphorylation levels of Akt1, Akt2, and S6 are significantly reduced in livers of db/db mice.
Biological Activity
Purity & Documentation
References
Customer Review
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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In Vitro | Dapagliflozin (0-10 μM;24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.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.. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability Assay
Western Blot Analysis
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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. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
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408.87 | |||||||||||||||||
C21H25ClO6 | |||||||||||||||||
461432-26-8 | |||||||||||||||||
Solid | |||||||||||||||||
White to off-white | |||||||||||||||||
O[C@H]1[C@H](C2=CC(CC3=CC=C(OCC)C=C3)=C(Cl)C=C2)O[C@H](CO)[C@@H](O)[C@@H]1O | |||||||||||||||||
Room temperature in continental US; may vary elsewhere. | |||||||||||||||||
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | |||||||||||||||||
In Vitro: 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
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. * 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo: Select the appropriate dissolution method based on your experimental animal and administration route. For the following dissolution methods, please ensure to first prepare a clear stock solution using an and then sequentially add co-solvents:
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.
In Vivo Dissolution Calculator Please enter the basic information of animal experiments: Dosage mg/kgAnimal weight Dosing volume 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). | |||||||||||||||||
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[1]. Pedersen MG, et al. Dapagliflozin stimulates glucagon secretion at high glucose: experiments and mathematical simulations of human A-cells. Sci Rep. 2016 Aug 18;6:31214.
[2]. Chiba Y, et al. Dapagliflozin, a Sodium-Glucose Co-Transporter 2 Inhibitor, Acutely Reduces Energy Expenditure in BAT via Neural Signals in Mice. PLoS One. 2016 Mar 10;11(3):e0150756.
[3]. Chang YK, et al. Dapagliflozin, SGLT2 Inhibitor, Attenuates Renal Ischemia-Reperfusion Injury. PLoS One. 2016 Jul 8;11(7):e0158810.
* 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 | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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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.
- Membrane Transporter/Ion Channel
- SGLT
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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Dapagliflozin461432-26-8BMS-512148BMS512148BMS 512148SGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit
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