ACETA potent and selective GluR5-containing kainate receptor antagonist

ACET (CAS 936095-50-0)

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Synonym: (S)-1-(2-Amino-2-carboxyethyl)-3-(2carboxy-5-phenylthiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
Application: A potent and selective GluR5-containing kainate receptor antagonist
CAS Number: 936095-50-0
Purity: ≥98%
Molecular Weight: 429.45
Molecular Formula: C20H19N3O6S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Potent and selective GluR5-containing kainate receptor antagonist (IC50 = 7 nM) that displays selectivity over GluR6-containing kainate, NMDA, AMPA and group I mGlu receptors. Reversibly blocks induction of NMDA recptor-independent long term potentiation (LTP) in vitro at nanomolar concentrations.


References

Dolman et al (2007) Synthesis and pharmacological characterisation of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. J.Med.Chem. 50 1558. Dargan et al (2009) ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function. Neuropharmacology 56 121.

Physical State :
Solid
Solubility :
Soluble in 100 mM NaOH (10 mM).
Storage :
Store at room temperature
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
SMILES :
Cc1cn(c(=O)n(c1=O)Cc2cc(sc2C(=O)O)c3ccccc3)C[C@@H](C(=O)O)N

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Certificate of Analysis

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