(+)-MK 801 Maleate (Synonyms: Dizocilpine Maleate) |
Catalog No.GC11025 |
Le (+)-MK 801 Maleate (MK-801 maléate) est un antagoniste puissant, sélectif et non compétitif des récepteurs NMDA avec une Kd de 37,2 nM dans les membranes cérébrales de rat.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 77086-22-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Primary mixed neuronal/glial cultures from fetal rat brains. |
Preparation method |
The solubility of this compound in DMSO is >16.9mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
10 μM for 30 minutes |
Applications |
NMDA induced apoptosis in mixed neuronal/glial cell cultures. In the presence of a mild excitotoxic insult, this investigation showed an attenuation of apoptotic cell death by MK 801. |
Animal experiment [2]: | |
Animal models |
C57BL/6; BALB/c mice |
Dosage form |
s.c. or i.p., 0.1 mg kg(-1) |
Application |
MK 801 in the chronically C57BL/6 chronic stress group that prevented weight gain deficit. For the C57BL/6 strain chronic MK 801 produced an alteration of the fur state. In the CA1 layer of chronically stressed C57BL/6 mice, MK 801 induced an increase of VGLUT1 immunoreactivity. For the BALB/c group, MK 801 enhanced BDNF mRNA in the chronic stress group in the DG. In the chronically stressed BALB/c mice, MK 801 prevented stressed induced VGLUT3 immunoreactivity up-regulation in the CA3 layer. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Wise-Faberowski L,Pearlstein RD,Warner DS., et al. NMDA-induced apoptosis in mixed neuronal/glial cortical cell cultures: the effects of isoflurane and dizocilpine. J Neurosurg Anesthesiol.2006 Oct;18(4):240-6. [2] .Farley S, Dumas S, El Mestikawy S ., et al. Increased expression of the Vesicular Glutamate Transporter-1 (VGLUT1) in the prefrontal cortex correlates with differential vulnerability to chronic stress in various mouse strains: effects of fluoxetine and MK-801. Neuropharmacology. 2012 Jan;62(1):503-17. |
(+)-MK 801 est un puissant antagoniste de NMDA avec une valeur Ki de 30,5 nM [1].
MK 801 est un puissant anticonvulsivant qui présente à la fois des propriétés anxiolytiques et sympathomimétiques. On a découvert qu'il était un antagoniste non compétitif de NMDA. MK 801 peut pénétrer dans le système nerveux central. Dans l'essai in vitro, MK 801 se lie aux membranes corticales cérébrales de rat avec une forte affinité de manière saturable. Cette liaison est réversible même lorsque la concentration de MK 801 atteint jusqu'à 100 μM. Il a également été constaté que cette liaison montre une spécificité régionale, la plupart des sites de liaison étant situés dans l'hippocampe. Dans les préparations en tranches corticales de rat, MK 801 provoque un blocage puissant des réponses dépolarisantes à NMDA avec une grande sélectivité. Cet effet est persistant et peut également entraîner une suppression de l'activité épileptiforme induite par la tétrodotoxine ou d'autres neurotoxines [1].
References:
[1] Wong EH, Kemp JA, Priestley T, Knight AR, Woodruff GN, Iversen LL . The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.
Cas No. | 77086-22-7 | SDF | |
Synonymes | Dizocilpine Maleate | ||
Chemical Name | (5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate | ||
Canonical SMILES | C[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4.O=C(O)/C=C\C(O)=O | ||
Formula | C20H19NO4 | M.Wt | 337.37 |
Solubility | ≥ 16.85mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL |
10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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