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

Dapagliflozin (Synonyms: BMS-512148)

Cat. No.: HY-10450 Purity: 99.96%
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Dapagliflozin (BMS-512148), a new type of drug 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

Dapagliflozin Chemical Structure

CAS No. : 461432-26-8

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Customer Review

Based on 10 publication(s) in Google Scholar

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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dapagliflozin (BMS-512148), a new type of drug 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[1]

    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]..

    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].

    Clinical Trial
    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

    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    40% PEG300    5% Tween-80    45% saline

      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    90% corn oil

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

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

    Purity: 99.96%

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    Product Name:
    Dapagliflozin
    Cat. No.:
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