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  5. Dizocilpine

Dizocilpine  (Synonyms: MK-801)

Cat. No.: HY-15084B Purity: 99.90%
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Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux.

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

Dizocilpine Chemical Structure

Dizocilpine Chemical Structure

CAS No. : 77086-21-6

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10 mg USD 70 In-stock
25 mg USD 140 In-stock
50 mg USD 250 In-stock
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Based on 30 publication(s) in Google Scholar

Other Forms of Dizocilpine:

Dizocilpine Related Antibodies

Top Publications Citing Use of Products

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2023 Mar 16;13(1):57.  [Abstract]

    Dizocilpine (MK-801; 1 mg/kg; i.v.; single) suppresses RIPC-induced SIRT3 upregulation in mice.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Aug;24(16):9287-9299.  [Abstract]

    Neurons are pre-treated with 10 μM Dizocilpine (MK801), followed by TNF-α treatment (40 ng/mL, 2 h). MK801 could attenuate TNF-α- induced intracellular calcium accumulation, phosphorylation of CAMK II and calpain-2, calpain activation and cathepsin B release as well as TrkB truncation.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450.  [Abstract]

    Western blot analysis confirms that MK-801 inhibits the decrease in GDF10 in SNL rats. The relative expression level of GDF10 in the SNL-vehicle group is significantly decreased, but remains unchanged in the SNL-MK-801 group versus sham.

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    Description

    Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux[1][2].

    IC50 & Target

    NMDA Receptor

     

    In Vitro

    Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches[3].
    Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells[4].

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

    Dizocilpine Related Antibodies
    In Vivo

    Dizocilpine maleate can be used to create schizophrenia models. An intraperitoneal injection of 0.2 mg/kg in SD rats results in a half-life of 52.31 minutes, an AUC of 3185.48 nM·min, and a clearance rate of 34 mL/min/kg[2].

    Induction of Schizophrenia
    Background
    The specific mechanism of schizophrenia induction is unclear. One hypothesis is that, Dizocilpine maleateleads to dysregulation of glutamatergic system through NMDA inhibition[2].
    Specific Mmodeling Methods
    Rat: Sprague-Dawley • male • adult with weight of 250-300 g
    Administration: 0.4 mg/kg • i.p. • single dose.
    Note
    Dizocilpine maleate is dissolved in 0.9% sterile saline.
    Modeling Indicators
    Behavior: Increased spontaneous activity with obvious anxiety-like behavior, increased motor activity in longer diatance (hyperactivity), reduced time staying in central area (avoidance of central area).
    Prepulse Inhibition (PPI): Decreased PPI significantly.
    maze test:Avoided open arm entries in elevated plus maze test and reduced number of novel arm entries in Y maze test.
    Correlated Product(s): Phencyclidine
    Opposite Product(s): Clozapine (HY-14539); Haloperidol (HY-14538)

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

    221.30

    Formula

    C16H15N
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@]1(N2)C3=CC=CC=C3C[C@]2([H])C4=CC=CC=C14
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (451.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.5188 mL 22.5938 mL 45.1875 mL
    5 mM 0.9038 mL 4.5188 mL 9.0375 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 5 mg/mL (22.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (22.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
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    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.
    Purity & Documentation
    References

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.5188 mL 22.5938 mL 45.1875 mL 112.9688 mL
    5 mM 0.9038 mL 4.5188 mL 9.0375 mL 22.5938 mL
    10 mM 0.4519 mL 2.2594 mL 4.5188 mL 11.2969 mL
    15 mM 0.3013 mL 1.5063 mL 3.0125 mL 7.5313 mL
    20 mM 0.2259 mL 1.1297 mL 2.2594 mL 5.6484 mL
    25 mM 0.1808 mL 0.9038 mL 1.8075 mL 4.5188 mL
    30 mM 0.1506 mL 0.7531 mL 1.5063 mL 3.7656 mL
    40 mM 0.1130 mL 0.5648 mL 1.1297 mL 2.8242 mL
    50 mM 0.0904 mL 0.4519 mL 0.9038 mL 2.2594 mL
    60 mM 0.0753 mL 0.3766 mL 0.7531 mL 1.8828 mL
    80 mM 0.0565 mL 0.2824 mL 0.5648 mL 1.4121 mL
    100 mM 0.0452 mL 0.2259 mL 0.4519 mL 1.1297 mL
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    Dizocilpine Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Dizocilpine77086-21-6MK-801MK801MK 801iGluRIonotropic glutamate receptorsnoncompetitiveambulationhyperlocomotionanticonvulsantneurotransmittervoltageInhibitorinhibitorinhibit

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