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Submit ReviewZK 200775
Description: Competitive non-NMDA iGluR antagonist
Alternative Names: MPQX
Chemical Name: [[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]phosphonic acid
Purity: ≥99% (HPLC)
Biological Activity for ZK 200775
ZK 200775 is a competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [3H]-AMPA (Ki = 120 nM) and [3H]-CNQX (Ki = 32 nM) binding sites and low affinity for kainate and NMDA channel-associated binding sites (IC50 values range from 2.5 to 11 μM). Inhibits currents induced by AMPA, Kainate and NMDA with IC50 values of 21 nM, 27 nM, and > 1 μM respectively. Displays anxiolytic, anticonvulsant and muscle relaxant activity in vivo.
Compound Libraries for ZK 200775
ZK 200775 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for ZK 200775
| M. Wt | 409.25 |
| Formula | C14H15N3O6F3P |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 161605-73-8 |
| PubChem ID | 208953 |
| InChI Key | WZMQMKNCWDCCMT-UHFFFAOYSA-N |
| Smiles | OP(O)(=O)CN1C(=O)C(=O)NC2=CC(=C(C=C12)N1CCOCC1)C(F)(F)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ZK 200775
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.93 | 100 | |
| ethanol | 20.46 | 50 |
Preparing Stock Solutions for ZK 200775
The following data is based on the product molecular weight 409.25. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.44 mL | 12.22 mL | 24.43 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.89 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets for ZK 200775
References for ZK 200775
References are publications that support the biological activity of the product.
Elger et al (2005) Novel α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration. J.Med.Chem. 48 4618 PMID: 15999999
Turski et al (1998) ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauman Proc.Natl.Acad.Sci.USA. 95 10960
Kosowski et al (2004) Nicotine-induced DA release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551n Pychopharmacology 175 114
Sobolevsky (2009) X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor. Nature 462 745 PMID: 19946266
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Keywords: ZK 200775, ZK 200775 supplier, Competitive, AMPA/kainate, antagonists, Glutamate, Receptors, iGluR, Ionotropic, ZK200775, MPQX, AMPA, Kainate, 2345, Tocris Bioscience
1 Citation for ZK 200775
Citations are publications that use Tocris products. Selected citations for ZK 200775 include:
Lesne et al (2005) Akt-dependent expression of NAIP-1 protects neurons against amyloid-{beta} toxicity. J Biol Chem 280 24941 PMID: 15797869
Do you know of a great paper that uses ZK 200775 from Tocris? Please let us know.
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