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Description: Potent and selective GluK1 kainate agonist
Chemical Name: (RS)-2-Amino-3-(3-hydroxy-5-tert-butylisoxazol-4-yl)propanoic acid
Purity: ≥98% (HPLC)
Biological Activity for ATPA
ATPA is a selective and potent GluK1 (formerly GluR5) kainate receptor agonist (Ki = 4.3 nM), inactive at GluK6 (formerly GluR6) (Ki > 1 mM) and only weakly active at AMPA receptors (GluA1-4) and the kainate receptors GluK5 (formerly KA-2) and GluK3 (formerly GluR7) (Ki values of 6 - 14 μM).
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
Technical Data for ATPA
| M. Wt | 228.25 |
| Formula | C10H16N2O4 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 140158-50-5 |
| PubChem ID | 2253 |
| InChI Key | PIXJURSCCVBKRF-UHFFFAOYSA-N |
| Smiles | CC(C)(C)C1=C(CC(N)C(O)=O)C(O)=NO1 |
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 ATPA
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 2.28 | 10 with gentle warming | |
| 1eq. NaOH | 4.57 | 20 with gentle warming |
Preparing Stock Solutions for ATPA
The following data is based on the product molecular weight 228.25. 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 |
|---|---|---|---|
| 0.2 mM | 21.91 mL | 109.53 mL | 219.06 mL |
| 1 mM | 4.38 mL | 21.91 mL | 43.81 mL |
| 2 mM | 2.19 mL | 10.95 mL | 21.91 mL |
| 10 mM | 0.44 mL | 2.19 mL | 4.38 mL |
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Product Datasheets for ATPA
References for ATPA
References are publications that support the biological activity of the product.
Clarke et al (1997) A hippocampal GluR5 kainate receptor regulating inhibitory synaptic transmission. Nature 389 599 PMID: 9335499
Matzen et al (1997) AMPA receptor agonists: synthesis, protolytic properties, and pharmacology of 3-isothiazole bioisasteres of glutamic acid. J.Med.Chem. 40 520 PMID: 9046343
Moldrich et al (1999) Excitotoxic injury profiles of low-affinity kainate receptor agonists in neuronal cultures. Eur.J.Pharmacol. 378 R1 PMID: 10478637
If you know of a relevant reference for ATPA, please let us know.
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Keywords: ATPA, ATPA supplier, Selective, potent, GluR5, agonists, Glutamate, Kainate, Receptors, iGlur, Ionotropic, GluK1, 1107, Tocris Bioscience
7 Citations for ATPA
Citations are publications that use Tocris products. Selected citations for ATPA include:
Song et al (2015) MinCyc does not affect long-term potentiation in the anterior cingulate cortex of normal adult mice. Front Pediatr 11 25 PMID: 25933605
Randall et al (2011) Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro. Eur J Neurosci 33 914 PMID: 21255131
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
Langner et al (2017) Kynurenic Acid Induces Impairment of Oligodendrocyte Viability: On the Role of Glutamatergic Mechanisms. Neurochem Res 42 838 PMID: 27444613
Talpalar and Kiehn (2010) Glutamatergic mechanisms for speed control and network operation in the rodent locomotor CpG. Front Neural Circuits 4 PMID: 20844601
Liu et al (2004) Astrocyte-mediated activation of neuronal kainate receptors. Mol Pain 101 3172 PMID: 14766987
Xu et al (2006) Presynaptic regulation of the inhibitory transmission by GluR5-containing kainate receptors in spinal substantia gelatinosa. Mol Pain 2 29 PMID: 16948848
Do you know of a great paper that uses ATPA from Tocris? Please let us know.
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