Biological Activity
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
ZK 200775 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.93 | 100 | |
| ethanol | 20.46 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 409.25. 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 | 2.44 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
References
References are publications that support the products' biological activity.
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 PMID:
Kosowski et al (2004) Nicotine-induced dopamine release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551n Pychopharmacology 175 114 PMID:
Sobolevsky (2009) X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor. Nature 462 745 PMID: 19946266
Keywords: ZK 200775, supplier, Competitive, AMPA/kainate, antagonists, Glutamate, Receptors, iGluR, Ionotropic, ZK200775, MPQX, AMPA, Receptors, Kainate, Receptors, AMPA, Receptors, Tocris Bioscience
