(-)-MK-801 maleate (Synonyms: (-)-Dizocilpine Maleate) |
Catalog No.GC15270
One-Click Copy Product Info
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(-)-MK 801 is a selective, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist (Ki = 211.7nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 121917-57-5
Sample solution is provided at 25 µL, 10mM.
(-)-MK 801 is a selective, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist (Ki = 211.7nM) [1]. (-)-MK 801 inhibits calcium influx into cells by physically blocking calcium (Ca²⁺) channels in the open state of NMDA receptors activated by glutamate and glycine [2-3]. (-)-MK 801 has anticonvulsant and neuroprotective properties [4].
In Panc-1 cells, cell proliferation was significantly inhibited by 1000μM (-)-MK 801 (0.1-1000μM; 48h) [5]. In HepG2 cells, (-)-MK 801 (62.5-500μM; 72h) inhibits cancer cell growth [6].
In sprague dawley rats, after (-)-MK 801 (0.2mg/kg; ip; 10d) treatment, rats showed impaired performance in multiple sensorimotor tests and developed severe symptoms of intoxication [7]. In albino mice, high-dose (-)-MK 801 (10mg/kg; ip; 5 months) treatment kills a small number of PC/RS cortical neurons in mice, leading to chronic learning impairment in spatial learning [8].
References:
[1]. Yang B, Ren Q, Ma M, et al. Antidepressant effects of (+)-MK-801 and (-)-MK-801 in the social defeat stress model[J]. International Journal of Neuropsychopharmacology, 2016, 19(12): pyw080.
[2]. Decollogne S, Tomas A, Lecerf C, et al. NMDA receptor complex blockade by oral administration of magnesium: comparison with MK-801[J]. Pharmacology Biochemistry and Behavior, 1997, 58(1): 261-268.
[3]. Song X, Jensen M Ø, Jogini V, et al. Mechanism of NMDA receptor channel block by MK-801 and memantine[J]. Biophysical Journal, 2018, 114(3): 24a-25a.
[4]. Urbańska E, Dziki M, Kleinrok Z, et al. Influence of MK-801 on the anticonvulsant activity of antiepileptics[J]. European journal of pharmacology, 1991, 200(2-3): 277-282.
[5]. Malsy M, Gebhardt K, Gruber M, et al. Effects of ketamine, s-ketamine, and MK 801 on proliferation, apoptosis, and necrosis in pancreatic cancer cells[J]. BMC anesthesiology, 2015, 15(1): 111.
[6]. Yamaguchi F, Hirata Y, Akram H, et al. FOXO/TXNIP pathway is involved in the suppression of hepatocellular carcinoma growth by glutamate antagonist MK-801[J]. BMC cancer, 2013, 13(1): 468.
[7]. Wozniak D F, Olney J W, Kettinger III L, et al. Behavioral effects of MK-801 in the rat[J]. Psychopharmacology, 1990, 101(1): 47-56.
[8]. Wozniak D F, Brosnan-Watters G, Nardi A, et al. MK-801 neurotoxicity in male mice: histologic effects and chronic impairment in spatial learning[J]. Brain research, 1996, 707(2): 165-179.
| Cell experiment [1]: | |
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Cell lines |
Panc-1 cells |
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Preparation Method |
Cells were incubated with 100μL of the test compounds for 48h (0.1-1000μM ketamine, s-ketamine, and (-)-MK 801). After 32h incubation, cells were additionally treated with BrdU labeling solution for the last 16h. The culture medium was removed, cells were fixed, and DNA was denatured. Afterwards, cells were incubated with Anti-BrdU-POD solution for 90min, and antibody conjugates were removed in three washing cycles. Immune complexes were detected by means of TMB substrate for 15min and quantified by measuring the absorbance at 405nm and 490nm. |
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Reaction Conditions |
0.1-1000μM; 48h |
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Applications |
In Panc-1 cells, cell proliferation was significantly inhibited by 1000μM (-)-MK 801. |
| Animal experiment [2]: | |
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Animal models |
Sprague dawley rats |
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Preparation Method |
(-)-MK 801 was dissolved in distilled water and adjusted to a neutral pH (7.3 +0.1) with NaOH. Drug challenge procedures commenced on day 31 and were carried out on every third day thereafter up to day 40. On day 31, five rats received injections of 0.2mg/kg (-)-MK 801 (injection volumes: 0.5mL) and five received saline. |
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Dosage form |
0.2mg/kg; ip; 10d |
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Applications |
After (-)-MK 801 treatment, rats showed impaired performance in multiple sensorimotor tests and developed severe symptoms of intoxication. |
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References: |
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| Cas No. | 121917-57-5 | SDF | |
| Synonyms | (-)-Dizocilpine Maleate | ||
| Canonical SMILES | C[C@@]1(N2)C3=CC=CC=C3C[C@H]2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O | ||
| Formula | C20H19NO4 | M.Wt | 337.37 |
| Solubility | ≥ 10.3mg/mL in DMSO | Storage | 4°C, sealed storage, away from moisture |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
| 5 mM | 592.8 μL | 2.9641 mL | 5.9282 mL |
| 10 mM | 296.4 μL | 1.4821 mL | 2.9641 mL |
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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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)