| Description |
Dapagliflozin is a new pharmacological therapy for type 2 diabetes, and inhibits sodium/glucose cotransporter 2 (SGLT2), which results in excretion of glucose into the urine. |
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| In Vitro |
Dapagliflozin pretreatment of hypoxic HK2 cells significantly improves the cell viability in a dose-dependent manner. Dapagliflozin decreases Bax expression, the Bax/Bcl2 ratio, and PARP expression in hypoxic HK2 cells[2]. |
| In Vivo |
At 11 mM glucose, dapagliflozin raises glucagon release from 18% to 32% of control, while the effect of dapagliflozin addition is minor at 1 mM glucose. At the intermediate glucose concentration of 6 mM, glucagon secretion is estimated to be 24% and 30% of control in the absence or presence of dapagliflozin, respectively[1]. Dapagliflozin pretreatment significantly reduces the number of TUNEL-positive cells in IR-injured kidneys. Dapagliflozin pretreatment significantly elevates the HIF1 expression in IR-injured renal tubular cells from mice[2]. Dapagliflozin (10 mg/kg, o.p.) causes a marked increase in urinary glucose in SGLT2i-mice. Dapagliflozin acutely suppresses BAT thermogenesis by reducing sympathetic nerve activity. Dapagliflozin enhances hepatic gluconeogenesis and glycogenolysis[3]. |
| Clinical Trial |
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| References |
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| Preparing Stock Solutions |
Please refer to the solubility information to select the appropriate solvent.
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| Cell Assay
[2] |
To perform the cell survival assay, cells are collected after 24 h incubation with vehicle or dapagliflozin pretreatment in 30-min ischemia and surviving cells are counted with Trypan blue staining. The percentage survival is determined by quantization of the relative viable number of treated cells divided by the viable number of untreated cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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| Animal Administration
[1] |
10-week-old male C57BL/6 mice weighing 30-33 g each are divided into five groups: vehicle (Vh)-treated sham (n=5), dapagliflozin-treated sham (n=5), Vh-treated IR (n=7), dapagliflozin-treated IR (n=7), and albendazole and dapagliflozin treated IR (n=7). Dapagliflozin is administrated via oral gavage at a dose of 10 mg/kg/day for 2 days, starting 24 h before surgery. Albendazole is injected subcutaneously 1 h before IR surgery. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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| References |
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| Molecular Weight |
408.87 |
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| Formula |
C₂₁H₂₅ClO₆ |
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| CAS No. |
461432-26-8 |
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| Storage |
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| Shipping | Room temperature in continental US; may vary elsewhere |
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| Solvent & Solubility |
10 mM in DMSO Dapagliflozin is prepared in 0.5 % CMC+distilled water (DW)[4]. * "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> |
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| References |
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Purity: 99.89%
COA (94 KB) LCMS (149 KB)
Handling Instructions (1252 KB)-
[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]. Yoon-Kyung Chang, et al. Dapagliflozin, SGLT2 Inhibitor, Attenuates Renal Ischemia-Reperfusion Injury. PLoS One. 2016; 11(7): e0158810.
[3]. 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.
[4]. Akahane K, et al. Efficacy of Mitiglinide Combined with Dapagliflozin in Streptozotocin-nicotinamide-induced Type 2 Diabetic Rats and in Zucker Fatty Rats. Drug Res (Stuttg). 2015 Aug;65(8):416-21.
