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  5. Dizocilpine

Dizocilpine  (Synonyms: MK-801)

製品番号: HY-15084B 純度: 99.95%
COA 取扱説明書 Technical Support

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.

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CAS 番号 : 77086-21-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 49 在庫あり
Solid
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10 mg $70 在庫あり
25 mg $140 在庫あり
50 mg $250 在庫あり
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カスタマーレビュー

Based on 44 publication(s) in Google Scholar

Other Forms of Dizocilpine:

Dizocilpine 関連抗体

Top Publications Citing Use of Products

顧客検証

Cell Migration/Invasion Assay
Flow Cytometry
In Vivo Efficacy Study
Histological Imaging/Staining
WB

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138.  [Abstract]

    The invasion assay was conducted using SUM159 cells (left) or 4T1 cells (right) treated with NAAG, MK801 (100 μM), or the combination.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138.  [Abstract]

    BMCs were treated with NAAG, MK801 (100 μM), or the combination for 5 d. The PMN-MDSC percentages in BMCs were analyzed using flow cytometry.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138.  [Abstract]

    BMCs were treated with NAAG, MK801 (100 μM), or the combination for 5 d. The cells were collected and lysed for Western blotting to detect ARG1 expression.

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138.  [Abstract]

    The tumor growth curve of 4T1 allograft mice treated with NAAG, MK801 (i.p., 1 mg/kg, 5 d a week), or the combination (n = 6).

    Dizocilpine purchased from MedChemExpress. Usage Cited in: Sci Bull. 2025 Apr 15;70(7):1126-1138.  [Abstract]

    HE staining of lungs from 4T1 tumor-bearing mice treated with NAAG, MK801 (i.p., 1 mg/kg, 5 d a week), or the combination. Representative images (left) and a bar graph (right) were shown. Scale bar, 200 μm.

    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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    AMPA Receptor NMDA Receptor Kainate Receptor

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    製品説明

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    MCF7 GI50
    > 300 μM
    Compound: MK-801
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay
    		[PMID: 30996788]
    Oocyte IC50
    29 nM
    Compound: MK-801
    Antagonist activity at NR2A transfected in oocytes
    Antagonist activity at NR2A transfected in oocytes
    		[PMID: 21524576]
    SK-BR-3 GI50
    > 300 μM
    Compound: MK-801
    Cytotoxicity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay
    Cytotoxicity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay
    		[PMID: 30996788]
    体外実験

    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 関連抗体
    体内実験

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    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 Modeling 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.
    分子量

    221.30

    分子式

    C16H15N
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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
    10 mM 0.4519 mL 2.2594 mL 4.5188 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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

    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.
    純度とドキュメンテーション

    純度: 99.95%

    COA (257 KB) HNMR (247 KB) RP-HPLC (246 KB) LCMS (94 KB)

    取扱説明書 (2659 KB)
    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, 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
    • No file chosen (Maximum size is: 1024 Kb)
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    Dizocilpine Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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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    製品名:
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    製品番号:
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