Biological Activity
A potent, selective and non-competitive NMDA receptor antagonist. Acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux. An effective anti-ischemic agent in several animal models. Part of the Mixed NMDA Receptor Tocriset™. (-)-MK 801 maleate (Cat. No. 0955) also available.
Compound Libraries
(+)-MK 801 maleate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 337.37 |
| Formula | C16H15N.C4H4O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 77086-22-7 |
| PubChem ID | 6420042 |
| InChI Key | QLTXKCWMEZIHBJ-PJGJYSAQSA-N |
| Smiles | O=C(O)/C=CC(O)=O.C[C@]1(N4)C3=C(C=CC=C3)C[C@@H]4C2=C1C=CC=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 33.74 | 100 | |
| ethanol | 16.87 | 50 | |
| water | 8.43 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 337.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.96 mL | 14.82 mL | 29.64 mL |
| 5 mM | 0.59 mL | 2.96 mL | 5.93 mL |
| 10 mM | 0.3 mL | 1.48 mL | 2.96 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.59 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Gill et al (1991) The neuroprotective action of dizocilpine (MK-801) in the rat middle cerebral artery occlusion model of focal ischaemia. Br.J.Pharmacol. 103 2030 PMID: 1912992
Hatfield et al (1992) The dose-response relationship and therapeutic window for dizocilpine (MK-801) in a rat focal ischaemia model. Eur.J.Pharmacol. 216 1 PMID: 1526248
Wong et al (1986) The anticonvulsant MK 801 is a potent N-methyl-D-aspartate antagonist. Proc.Natl.Acad.Sci.U.S.A. 83 7104 PMID: 3529096
Zajaczkowski et al (1997) Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP. Neuropharmacology 36 961 PMID: 9257940
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