Biological Activity
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 receptor-independent long term potentiation (LTP) in vitro at nanomolar concentrations.
Technical Data
| M. Wt | 429.45 |
| Formula | C20H19N3O6S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 936095-50-0 |
| PubChem ID | 16125102 |
| InChI Key | LCZDCKMQSBGXAH-AWEZNQCLSA-N |
| Smiles | O=C(C(C)=CN1C[C@@H](C(O)=O)N)N(CC2=C(C(O)=O)SC(C3=CC=CC=C3)=C2)C1=O |
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 | |||
| 3eq. NaOH | 8.59 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 429.45. 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 | 2.33 mL | 11.64 mL | 23.29 mL |
| 5 mM | 0.47 mL | 2.33 mL | 4.66 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 antagonis J.Med.Chem. 50 1558 PMID: 17348638
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 PMID: 18789344
Keywords: ACET, supplier, Potent, antagonists, GluR5-containing, kainate, receptors, Glutamate, Kainate, Receptors, iGluR, Ionotropic, Kainate, Receptors, Kainate, Receptors, Tocris Bioscience
