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Description: Potent kainate antagonist; displays selectivity for GluK1-containing receptors
Chemical Name: (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-5-phenylthiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
Purity: ≥98% (HPLC)
Biological Activity for ACET
ACET is a potent and selective GluK1 (formerly GluR5) containing kainate receptor antagonist (IC50 = 7 nM) that displays selectivity over GluK2 (formerly 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.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data for ACET
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for ACET
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.59 | 20 | |
| 3eq. NaOH | 4.29 | 10 |
Preparing Stock Solutions for ACET
The following data is based on the product molecular weight 429.45. 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 |
|---|---|---|---|
| 0.2 mM | 11.64 mL | 58.21 mL | 116.43 mL |
| 1 mM | 2.33 mL | 11.64 mL | 23.29 mL |
| 2 mM | 1.16 mL | 5.82 mL | 11.64 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
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Product Datasheets for ACET
References for ACET
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for ACET, please let us know.
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Keywords: ACET, ACET supplier, Potent, antagonists, GluR5-containing, kainate, receptors, Glutamate, Kainate, Receptors, iGluR, Ionotropic, GluK1, 2728, Tocris Bioscience
2 Citations for ACET
Citations are publications that use Tocris products. Selected citations for ACET include:
Granger and Nicoll (2014) LTD expression is independent of glutamate receptor subtype. J Virol 6 15 PMID: 25071549
Kiyama et al (2019) Essential Roles of Tbr1 in the Formation and Maintenance of the Orientation-Selective J-RGCs and a Group of OFF-Sustained RGCs in Mouse. Cell Rep 27 900 PMID: 30995485
Do you know of a great paper that uses ACET from Tocris? Please let us know.
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