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Purity: ≥98%
(-)-Dizocilpine Maleate [also known as (-)-MK-801; MK801; MK 801], the maleate salt of dizocilpine, is a novel, potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potential to treat a wide range of neurodegenerative conditions or disorders in which NMDA receptors play an important role. Dizocilpine inhibits NMDA with a Ki of 30.5 nM, and shows potent anti-convulsant, anti-anxiolytic and sympathomimetic activities. MK 801 can penetrate into the central nervous system. In the in vitro assay, MK 801 binds to rat cerebral cortical membrane with high affinity in a saturable manner.
| ln Vitro |
In HEK cells, (-)-Dizocilpine maleate ((-)-MK-801 maleate) dramatically reduced the uptake of all three monoamine transporters (dopamine, serotonin, and norepinephrine) in a dose-dependent manner. On the norepinephrine, dopamine, and serotonin transporters, (-)-Dizocilpine has Ki values of 3.7 μM, 40 μM, and 47 μM, respectively[2].
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| ln Vivo |
In the social defeat stress model, (-)-Dizocilpine maleate (0.1 mg/kg; intraperitoneal injection; male adult C57BL/6 mice) therapy produces fast antidepressant effects[1].
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| Animal Protocol |
Animal/Disease Models: Male adult C57BL/6 mice ( 20-25g ; aged 8 weeks) with social defeat stress model[1]
Doses: 0.1 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Induced rapid antidepressant effects in the social defeat stress model. |
| References |
[1]. Yang B, et al. Antidepressant Effects of (+)-MK-801 and (-)-MK-801 in the Social Defeat Stress Model. Int J Neuropsychopharmacol. 2016 Dec 30;19(12).
[2]. Nishimura M, et al. MK-801 blocks monoamine transporters expressed in HEK cells. FEBS Lett. 1998 Feb 27;423(3):376-80. |
| Molecular Formula |
C20H19NO4
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| Molecular Weight |
337.37
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| CAS # |
121917-57-5
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| Related CAS # |
Dizocilpine maleate;77086-22-7;Dizocilpine;77086-21-6
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| SMILES |
C[C@@]1(N2)C3=CC=CC=C3C[C@H]2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.41 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.08 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: 30% PEG400+0.5% Tween80+5% propylene glycol:15 mg/mL Solubility in Formulation 8: 4.55 mg/mL (13.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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