1. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Autophagy
  2. Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein
  3. Glibenclamide

グリベンクラミド  (Synonyms: Glibenclamide; Glyburide)

製品番号: HY-15206 純度: 99.83%
COA 取扱説明書 Technical Support

Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.

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CAS 番号 : 10238-21-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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カスタマーレビュー

Based on 27 publication(s) in Google Scholar

Other Forms of Glibenclamide:

Top Publications Citing Use of Products

    Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212.  [Abstract]

    Immunoblots of DARTS assay that verified the binding of glyburide (50 µM, 24 h) to IFI16 in U251 cells (n = 3). An unpaired two-tailed t-test was applied. Data are presented as mean ± SD.

    Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212.  [Abstract]

    Time response of the mice weight after implantation of U251R cells, on average, the xenograft was locally irradiated with 15 Gy of X-rays, and the mice were administered intragastrically with 1 mg/kg glyburide 2 h before irradiation (N = 5 per group). Data are presented as mean ± SD.

    Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212.  [Abstract]

    Representative MRI images of U251R xenografts by T2-weighted MRI at 10-day and 20-day after cell implantation, the whole mount HE-stained brain sections of mice (administered intragastrically with 1 mg/kg glyburide 2 h before irradiation).

    Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212.  [Abstract]

    Glyburide (administered intragastrically with 1 mg/kg glyburide 2 h before irradiation). The positive area of IFI16, HMOX1, and GPX4 in the U251R tumor tissues (N = 5 per group). An unpaired two-tailed t-test was applied. Data are presented as mean ± SD. “n” means the number of individual experiments. “N” represents the number of mice analyzed.

    Glibenclamide purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2020 Mar;153:104679.  [Abstract]

    Glucose-dependent insulinotropic effects of CPU025 in MIN6 cells. MIN6 cells were treated with 2 or 25 mM glucose in the absence or presence of Glibenclamide (3 μM).

    Glibenclamide purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 May 12;8:269.  [Abstract]

    The inhibition of HSP70 releasing by Glibenclamide suppresses morphine-induced ER stress and the phosphorylation of PKA and NR-1. Glibenclamide (200 μM) inhibits the decrease of intracellular HSP70 caused by morphine in SH-SY5Y cells.
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    製品説明

    Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].

    IC50 & Target

    KATP[1]

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    0.0043 3
    Compound: 6 (glyburide)
    Inhibition of human SUR1/Kir6.2 expressed in CHO cells
    Inhibition of human SUR1/Kir6.2 expressed in CHO cells
    [PMID: 11356099]
    CHO IC50
    15 3
    Compound: glibenclamide
    Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
    Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
    [PMID: 21397997]
    CHO IC50
    15 3
    Compound: glibenclamide
    Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
    Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
    [PMID: 21397997]
    HEK293 IC50
    1.4 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    [PMID: 22587986]
    CHO IC50
    0.0043 3
    Compound: 6 (glyburide)
    Inhibition of human SUR1/Kir6.2 expressed in CHO cells
    Inhibition of human SUR1/Kir6.2 expressed in CHO cells
    [PMID: 11356099]
    CHO IC50
    15 3
    Compound: glibenclamide
    Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
    Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
    [PMID: 21397997]
    HEK293 IC50
    2.2 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    [PMID: 22587986]
    HEK293 IC50
    1.4 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    [PMID: 22587986]
    HEK293 IC50
    21 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    [PMID: 22587986]
    HEK293 IC50
    21 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    [PMID: 22587986]
    HEK293 IC50
    2.2 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    [PMID: 22587986]
    INS-1E EC50
    0.003 3
    Compound: glibenclamide
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
    [PMID: 24484900]
    INS-1E EC50
    0.007 3
    Compound: glibenclamide
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
    [PMID: 24484900]
    INS-1E EC50
    0.007 3
    Compound: glibenclamide
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
    [PMID: 24484900]
    INS-1E EC50
    0.003 3
    Compound: glibenclamide
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
    [PMID: 24484900]
    Mesenchymal stem cells EC50
    2.8 3
    Compound: GLI
    Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
    Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
    [PMID: 35172097]
    Mesenchymal stem cells EC50
    2.8 3
    Compound: GLI
    Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
    Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
    [PMID: 35172097]
    U-373MG ATCC IC50
    > 100 3
    Compound: Glibenclamide
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    [PMID: 22809560]
    Oocyte IC50
    0.22 3
    Compound: 6 (glyburide)
    Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
    Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
    [PMID: 11356099]
    Sf21 IC50
    5.3 3
    Compound: Glibenclamide
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Sf21 IC50
    2.8 3
    Compound: Glibenclamide
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    T-cell line IC50
    1 3
    Compound: 2
    In vitro inhibition of Rb efflux in human T-cells; 1-10
    In vitro inhibition of Rb efflux in human T-cells; 1-10
    10.1016/S0960-894X(97)00163-7
    U-373MG ATCC IC50
    >100 3
    Compound: Glibenclamide
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    [PMID: 22809560]
    HEK293 IC50
    1.4 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
    [PMID: 22587986]
    HEK293 IC50
    2.2 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
    [PMID: 22587986]
    HEK293 IC50
    21 3
    Compound: Glibenclamide
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
    [PMID: 22587986]
    INS-1E EC50
    0.003 3
    Compound: glibenclamide
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
    [PMID: 24484900]
    INS-1E EC50
    0.007 3
    Compound: glibenclamide
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
    Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
    [PMID: 24484900]
    Mesenchymal stem cells EC50
    2.8 3
    Compound: GLI
    Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
    Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
    [PMID: 35172097]
    Oocyte IC50
    0.22 3
    Compound: 6 (glyburide)
    Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
    Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
    [PMID: 11356099]
    Sf21 IC50
    2.8 3
    Compound: Glibenclamide
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Sf21 IC50
    5.3 3
    Compound: Glibenclamide
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    T-cell line IC50
    1 3
    Compound: 2
    In vitro inhibition of Rb efflux in human T-cells; 1-10
    In vitro inhibition of Rb efflux in human T-cells; 1-10
    10.1016/S0960-894X(97)00163-7
    U-373MG ATCC IC50
    > 100 3
    Compound: Glibenclamide
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    Growth inhibition of human U373 cells after 72 hrs by MTT assay
    [PMID: 22809560]
    体外実験

    Glibenclamide (Brown adipocytes; 10 μΜ; 1 day) has no effect on adipocyte differentiation. Glibenclamide (Ucp1-2A-GFP brown adipocyte) significantly increases UCP1 expression. Glibenclamide directly binds and blocks the SUR1 subunits of ATP-dependent potassium channels (KATP) and consequently increases insulin secretion from the pancreatic β cells[2]. Glibenclamide interferes with mitochondrial bioenergy by permeating mitochondrial intima with Cl- and promoting mitochondrial net Cl-/K+ cotransport[4]. Glibenclamide induced autophagy inhibits its insulin secretion-improving function in β cells[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    体内実験

    Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level[2].
    Glibenclamide (50 μg/kg; p.o.) does not cause significant change, such as body weight or body composition[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Mice[2]
    Dosage: 2 mg/kg
    Administration: P.o.
    Result: Increased of insulin release and rapid drop of blood glucose level.
    分子量

    494.00

    分子式

    C23H28ClN3O5S

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC(C(NCCC2=CC=C(S(NC(NC3CCCCC3)=O)(=O)=O)C=C2)=O)=C(OC)C=C1

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (202.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0243 mL 10.1215 mL 20.2429 mL
    5 mM 0.4049 mL 2.0243 mL 4.0486 mL
    10 mM 0.2024 mL 1.0121 mL 2.0243 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (5.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    純度とドキュメンテーション

    純度: 99.83%

    参考文献

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0243 mL 10.1215 mL 20.2429 mL 50.6073 mL
    5 mM 0.4049 mL 2.0243 mL 4.0486 mL 10.1215 mL
    10 mM 0.2024 mL 1.0121 mL 2.0243 mL 5.0607 mL
    15 mM 0.1350 mL 0.6748 mL 1.3495 mL 3.3738 mL
    20 mM 0.1012 mL 0.5061 mL 1.0121 mL 2.5304 mL
    25 mM 0.0810 mL 0.4049 mL 0.8097 mL 2.0243 mL
    30 mM 0.0675 mL 0.3374 mL 0.6748 mL 1.6869 mL
    40 mM 0.0506 mL 0.2530 mL 0.5061 mL 1.2652 mL
    50 mM 0.0405 mL 0.2024 mL 0.4049 mL 1.0121 mL
    60 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8435 mL
    80 mM 0.0253 mL 0.1265 mL 0.2530 mL 0.6326 mL
    100 mM 0.0202 mL 0.1012 mL 0.2024 mL 0.5061 mL
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    製品名:
    Glibenclamide
    製品番号:
    HY-15206
    数量:
    MCE 日本正規代理店: