1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. Dizocilpine Maleate

Dizocilpine Maleate (Synonyms: (+)-MK 801 (Maleate))

Cat. No.: HY-15084 Purity: 99.98%
Handling Instructions

Dizocilpine ((+)-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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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 222 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Dizocilpine Maleate:

Top Publications Citing Use of Products

    Dizocilpine Maleate purchased from MCE. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450.

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Dizocilpine ((+)-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

    Ki: 37.2 nM (NMDA receptor, in rat brain membrane)[1]

    In Vitro

    [3H]MK-801 binds with NMDA receptor with a Kd of 37.2 ±2.7 nM in rat cerebral cortical membranes[1]. Dizocilpine ((+)-MK 801) shows an inhibitory activity against N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50s of 20 nM and 9 nM, respectively[2]. Dizocilpine ((+)-MK 801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine ((+)-MK 801) from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 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. MK-801 (< 500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells[4].

    In Vivo

    Dizocilpine ((+)-MK 801) (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 ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine ((+)-MK 801) (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement[5].

    Molecular Weight

    337.37

    Formula

    C₂₀H₁₉NO₄

    CAS No.

    77086-22-7

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (296.41 mM; Need ultrasonic)

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

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.2964 mL 1.4821 mL 2.9641 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    • 4.

      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

    • 5.

      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

    • 6.

      Add each solvent one by one:  10% EtOH    90% corn oil

      Solubility: 2.5 mg/mL (7.41 mM); Precipitated solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    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
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    Product Name:
    Dizocilpine Maleate
    Cat. No.:
    HY-15084
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