ZK 200775

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Cat.No. 2345 - ZK 200775 | C14H15N3O6F3P | CAS No. 161605-73-8
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)
Datasheet
Citations (1)
Reviews
Literature

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

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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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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 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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References

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


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*Please note that Tocris will only send literature to established scientific business / institute addresses.


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