1. Membrane Transporter/Ion Channel
  2. SGLT
  3. Dapagliflozin

Dapagliflozin (Synonyms: BMS-512148)

Cat. No.: HY-10450 Purity: 99.85%
Handling Instructions

Dapagliflozin (BMS-512148) is a sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

For research use only. We do not sell to patients.

Dapagliflozin Chemical Structure

Dapagliflozin Chemical Structure

CAS No. : 461432-26-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 110 In-stock
Estimated Time of Arrival: December 31
100 mg USD 140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of Dapagliflozin:

Top Publications Citing Use of Products

    Dapagliflozin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Jun;152:45-59.

    Effects of Dapagliflozin and Empagliflozin on p62 expression in LPS-untreated and LPS-treated RAW264.7 cells.

    Dapagliflozin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;45(5):1747-1758.

    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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dapagliflozin (BMS-512148) is a sodium-glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

    IC50 & Target

    SGLT2[1]

    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
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (244.58 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    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.

    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.

    References
    Molecular Weight

    408.87

    Formula

    C₂₁H₂₅ClO₆

    CAS No.

    461432-26-8

    SMILES

    O[[email protected]]1[[email protected]](C2=CC(CC3=CC=C(OCC)C=C3)=C(Cl)C=C2)O[[email protected]](CO)[[email protected]@H](O)[[email protected]@H]1O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.85%

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    Product Name:
    Dapagliflozin
    Cat. No.:
    HY-10450
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    Dapagliflozin

    Cat. No.: HY-10450