1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR

(+)-MK 801 Maleate (Synonyms: Dizocilpine maleate; Dizocilpine hydrogen maleate; (+)-MK 801; MK 801)

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

(+)-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.
(+)-MK 801 Maleate Chemical Structure

(+)-MK 801 Maleate Chemical Structure

CAS No. : 77086-22-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
10 mg USD 60 In-stock
50 mg USD 222 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of (+)-MK 801 Maleate:

    (+)-MK 801 Maleate purchased from MCE. Usage Cited in: Neuroreport. 2017 May 24;28(8):444-450.

    Western blot results further confirm the decrease in GDF10 expression induced by NMDA.

    (+)-MK 801 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

    • Technical Information

    • Purity & Documentation

    • References

    Description

    (+)-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: 30.5 nM

    In Vitro

    [3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for [3H]MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype[1]. MK-801 inhibits N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively[2]. MK-801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg2+ (10 mM) prevents 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 is also effective at blocking NMDA-activated single-channel activity in outside-out patches[3]. MK-801 (< 500 μM) prevents LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells[4]

    In Vivo

    Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice[4]. MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement[5]

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [1]

    Cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold 0.32mol/Lsucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1×103 g, and the supernatant is recentrifuged at 1×104 g for 20 min at 4°C. The pellet is suspended in assay buffer (118 mM NaCl/4.7 mM KCl/1.2mM MgSO4/5 mM NaHCO3/20 mM Hepes/1.2 mM KH2PO4/2.5 mM CaCl2/11 mM glucose, pH 7.4) and incubated at 23°C for 20 min prior to final centrifugation at 1×103 g for 20 min at 4°C. The pellet is resuspended in assay buffer (70 mL per gram of original tissue). Binding of [3H]MK-801 is measured by incubating 750 μL duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 μL of buffer containing displacer or of buffer alone (total binding), 100 μL of 50 nM [3H]MK-801, and 50 μL of buffer for 60 min at 23°C. Nonspecific binding is defined by 100 μM (final concentration) unlabeled MK-801. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [5]

    MK-801 is formulated in saline.

    Animals are given saline or 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 MK-801 to disrupt reconsolidation. Animals undergo preconditioning, conditioning, testing, and extinction but animals are injected with saline or 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 MK-801. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO; Ethanol:6 mg/mL; H2O:< 0.6 mg/mL

    MK-801 is dissolved in 1% dimethyl sulfoxide and diluted with preservative-free normal saline at a concentration of 2 μg/μL[6].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.98%

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    Product Name:
    (+)-MK 801 Maleate
    Cat. No.:
    HY-15084
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