1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. (-)-Dizocilpine maleate

(-)-Dizocilpine maleate (Synonyms: (-)-MK-801 maleate)

Cat. No.: HY-15084A Purity: 99.84%
Handling Instructions

(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects.

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

(-)-Dizocilpine maleate Chemical Structure

(-)-Dizocilpine maleate Chemical Structure

CAS No. : 121917-57-5

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
10 mg USD 55 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 280 In-stock
Estimated Time of Arrival: December 31
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Description

(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects[1][2].

IC50 & Target

Ki: 211.7 nM (N-methyl-D-aspartate (NMDA) receptor)[1]

In Vitro

(-)-Dizocilpine maleate ((-)-MK-801 maleate) significantly inhibited the uptake of all three (norepinephrine, dopamine and serotonin) monoamine transporters in a dose-dependent manner in HEK cells. The Ki values of (-)-Dizocilpine on the norepinephrine, dopamine and serotonin transporters are 3.7 μM, 40 μM and 47 μM, respectively[2].

In Vivo

(-)-Dizocilpine maleate (0.1 mg/kg; intraperitoneal injection; male adult C57BL/6 mice) treatment induces rapid antidepressant effects in the social defeat stress model[1].

Animal Model: Male adult C57BL/6 mice ( 20-25g; aged 8 weeks) with social defeat stress model[1]
Dosage: 0.1 mg/kg
Administration: Intraperitoneal injection
Result: Induced rapid antidepressant effects in the social defeat stress model.
Molecular Weight

337.37

Formula

C₂₀H₁₉NO₄

CAS No.

121917-57-5

SMILES

C[[email protected]@]1(N2)C3=CC=CC=C3C[[email protected]]2C4=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)

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: ≥ 10 mg/mL (29.64 mM); Clear solution

  • 2.

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

    Solubility: ≥ 10 mg/mL (29.64 mM); Clear solution

  • 3.

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

    Solubility: ≥ 10 mg/mL (29.64 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); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.84%

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Keywords:

(-)-Dizocilpine(-)-MK-801iGluRIonotropic glutamate receptorsDizocilpine(-)-enantiomerNMDAantidepressantless-activemonoaminetransportersInhibitorinhibitorinhibit

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(-)-Dizocilpine maleate
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