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> Glibenclamide [10238-21-8]

Glibenclamide [10238-21-8]

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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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Glibenclamide Estructura química

Glibenclamide Estructura química

No. CAS : 10238-21-8

This product is a controlled substance and not for sale in your territory.

Based on 20 publication(s) in Google Scholar

Other Forms of Glibenclamide:

  • Glyburide-d11 Obtener un presupuesto
  • Glyburide-d3 Obtener un presupuesto
  • Glibenclamide potassium Obtener un presupuesto
  • Glibenclamide (Standard) Obtener un presupuesto

    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.
    Descripciòn

    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]
    In Vitro

    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.

    Glibenclamide Related Antibodies
    In Vivo

    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.
    Ensayo clínico
    Peso molecular

    494.00

    Fòrmula

    C23H28ClN3O5S
    No. CAS

    10238-21-8
    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
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    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
    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.

    • Calculadora de molaridad

    • Calculadora de dilución

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • 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.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Pureza y Documentación

    Purity: 99.94%

    COA (247 KB) HNMR (282 KB) RP-HPLC (242 KB) LCMS (86 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    • [1]. Heo R, et al. The anti-diabetic drug trelagliptin induces vasodilation via activation of Kv channels and SERCA pumps. Life Sci. 2021;283:119868.  [Content Brief]

      [2]. Qiu Y, et al. Glyburide Regulates UCP1 Expression in Adipocytes Independent of KATP Channel Blockade. iScience. 2020;23(9):101446.  [Content Brief]

      [3]. Golstein PE, et al. P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999;437(5):652-660.  [Content Brief]

      [4]. Fernandes MA, et al. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. J Biochem Mol Toxicol. 2004;18(3):162-169.  [Content Brief]

      [5]. Zhou J, et al. Glibenclamide-Induced Autophagy Inhibits Its Insulin Secretion-Improving Function in β Cells. Int J Endocrinol. 2019;2019:1265175.  [Content Brief]

    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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    Glibenclamide Related Classifications

    Help & FAQs

    Keywords:

    Glibenclamide10238-21-8GlyburidePotassium ChannelMitochondrial MetabolismAutophagyCFTRP-glycoproteinKcsACystic fibrosis transmembrane conductance regulatorP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243ATP-sensitivediabetesobesitySUR1cysticfibrosistransmembraneconductanceregulatormitochondrialbioenergeticsautophagyadipocytesInhibitorinhibitorinhibit

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