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  5. Dizocilpine maleate

Dizocilpine maleate  (Synonyms: MK-801 maleate)

Cat. No.: HY-15084 Purity: 99.94%
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Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

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

Dizocilpine maleate Chemical Structure

Dizocilpine maleate Chemical Structure

CAS No. : 77086-22-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mg USD 66 In-stock
50 mg USD 244 In-stock
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Based on 28 publication(s) in Google Scholar

Other Forms of Dizocilpine maleate:

Dizocilpine maleate Related Antibodies

Top Publications Citing Use of Products

    Dizocilpine maleate 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 maleate 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 maleate 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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    • References

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    Description

    Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.

    IC50 & Target

    NMDA Receptor

     

    In Vitro

    [3H]Dizocilpine maleate binds with NMDA receptor with a Kd of 37.2±2.7 nM in rat cerebral cortical membranes[1].
    Dizocilpine maleate causes a progressive, long-lasting blockade of current induced by N-Me-D-Asp[3].
    Dizocilpine maleate progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine (MK-801) is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches[3].
    Dizocilpine maleate (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (MK-801; <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 maleate Related Antibodies
    In Vivo

    Dizocilpine maleate can be used in animal modeling to construct models of schizophrenia. Dizocilpine maleate (MK 801 maleate) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice[4].
    Dizocilpine maleate (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine maleate (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement[5].
    Dizocilpine maleate (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg, but not at 0.03 and 0.1 mg/kg[6].Dizocilpine maleate (0.2 mg/kg, i.p.) exhibits a half-time of 52.31 min, an AUC of 3185.48 nM·min and a clearance of 34 nM in Sprague-Dawley rats[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
    Rats: Sprague-Dawley • male • adult with weight of 250-300 g
    Administration: 0.4 mg/kg • i.p. • single dose.


    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

    337.37

    Formula

    C20H19NO4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    C[C@]12C3=CC=CC=C3C[C@@H](N2)C4=CC=CC=C14.O=C(O)/C=C\C(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 133.33 mg/mL (395.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 25 mg/mL (74.10 mM; Need ultrasonic)

    H2O : 7.69 mg/mL (22.79 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9641 mL 14.8205 mL 29.6410 mL
    5 mM 0.5928 mL 2.9641 mL 5.9282 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.41 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 EtOH 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.41 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 EtOH stock solution (25.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  Saline

      Solubility: 3.45 mg/mL (10.23 mM); Clear solution; Need ultrasonic

    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).

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    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

    Purity: 99.94%

    COA (261 KB) HNMR (281 KB) LCMS (89 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [5]

    Animals are given saline or Dizocilpine ((+)-MK 801) followed by cocaine 30 min later in the home cage instead of in the CPP apparatus for the two days of “reactivation.” This is done to determine whether reactivation of the memory for the cocaine-associated context by cocaine in the CPP context is necessary for the ability of Dizocilpine ((+)-MK 801) to disrupt reconsolidation. Animals undergo preconditioning, conditioning, testing, and extinction but animals are injected with saline or Dizocilpine ((+)-MK 801) (0.20 mg/kg, i.p.) 30 min prior to a cocaine injection (10 mg/kg, i.p.) in the home cage. Animals remain in the home cages, and the next day, the procedure from the first day of reactivation is repeated. The following day, animals are tested for cocaine-primed reinstatement in their CPP box without any prior microinjection of saline or Dizocilpine ((+)-MK 801).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 2 years; -20°C, 1 year (sealed storage, away from moisture). 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
    H2O / Ethanol / DMSO 1 mM 2.9641 mL 14.8205 mL 29.6410 mL 74.1026 mL
    5 mM 0.5928 mL 2.9641 mL 5.9282 mL 14.8205 mL
    10 mM 0.2964 mL 1.4821 mL 2.9641 mL 7.4103 mL
    15 mM 0.1976 mL 0.9880 mL 1.9761 mL 4.9402 mL
    20 mM 0.1482 mL 0.7410 mL 1.4821 mL 3.7051 mL
    Ethanol / DMSO 25 mM 0.1186 mL 0.5928 mL 1.1856 mL 2.9641 mL
    30 mM 0.0988 mL 0.4940 mL 0.9880 mL 2.4701 mL
    40 mM 0.0741 mL 0.3705 mL 0.7410 mL 1.8526 mL
    50 mM 0.0593 mL 0.2964 mL 0.5928 mL 1.4821 mL
    60 mM 0.0494 mL 0.2470 mL 0.4940 mL 1.2350 mL
    DMSO 80 mM 0.0371 mL 0.1853 mL 0.3705 mL 0.9263 mL
    100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7410 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Dizocilpine maleate Related Classifications

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    • 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:

    Dizocilpine77086-22-7MK-801MK801MK 801iGluRIonotropic glutamate receptorsnoncompetitiveambulationhyperlocomotionanticonvulsantneurotransmittervoltageInhibitorinhibitorinhibit

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