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Biological Activity for L-trans-2,4-PDC
L-trans-2,4-PDC is a potent, competitive, transportable EAAT1-4 inhibitor/non-transportable EAAT5 inhibitor. In [3H]-d-Asp uptake assays in HEK293 cells expressing human EAAT1, EAAT2 and EAAT3, Ki values are 20, 20 and 109 μM, respectively. In a FLIPR Membrane Potential (FMP) assay, Km values for L-trans-2,4-PDC are 7.7, 11 and 19 μM for human EAAT2, EAAT3 and EAAT1, respectively.
Technical Data for L-trans-2,4-PDC
|Storage||Store at RT|
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 L-trans-2,4-PDC
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for L-trans-2,4-PDC
The following data is based on the product molecular weight 159.14. 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||6.28 mL||31.42 mL||62.84 mL|
|5 mM||1.26 mL||6.28 mL||12.57 mL|
|10 mM||0.63 mL||3.14 mL||6.28 mL|
|50 mM||0.13 mL||0.63 mL||1.26 mL|
References for L-trans-2,4-PDC
References are publications that support the biological activity of the product.
Bridges et al (1991) Conformationally defined neurotransmitter analogues. Selective inhibition of glutamate uptake by one pyrrolidine-2,4-dicarboxylate diastereomer. J.Med.Chem. 34 717 PMID: 1671706
Mitrovic and Johnston (1994) Regional differences in the inhibition of L-glutamate amd L-aspartate sodium-dependent high affinity uptake systems in rat CNS synaptosomes by L-trans-pyrrolidine-2,4-dicarboxylic threo-3-hydroxy-D-aspartate and D-aspartate. Neurochem.Int. 24 583 PMID: 7981641
Zuiderwijk et al (1996) Effects of uptake carrier blockers SK & F 89976-A and L-trans-PDC on in vivo release of amino acids in rat hippocampus. Eur.J.Pharmacol. 307 275 PMID: 8836615
Jensen and Bräuner-Osborne (2004) Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay. Biochem.Pharmacol. 67 2115 PMID: 15135308
If you know of a relevant reference for L-trans-2,4-PDC, please let us know.
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Keywords: L-trans-2,4-PDC, L-trans-2,4-PDC supplier, potent, competitive, Transportable, EAAT1-4, EAAT2, EAAT3, EAAT4, inhibitors, inhibits, non-transportable, EAAT5, EAAT, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, reuptake, trans-4-Carboxy-L-proline, Acids, 0298, Tocris Bioscience
4 Citations for L-trans-2,4-PDC
Citations are publications that use Tocris products. Selected citations for L-trans-2,4-PDC include:
Beaulé et al (2009) Circadian modulation of gene expression, but not glutamate uptake, in mouse and rat cortical astrocytes. PLoS One 4 e7476 PMID: 19829696
Yin and Weiss (2012) Marked synergism between mutant SOD1 and glutamate transport inhibition in the induction of motor neuronal degeneration in spinal cord slice cultures. Brain Res 1448 153 PMID: 22370146
Heinrich et al (2012) K+ depolarization evokes ATP, adenosine and glutamate release from glia in rat hippocampus: a microelectrode biosensor study. Br J Pharmacol 167 1003 PMID: 22394324
Young et al (2007) Glutamate receptor expression and chronic glutamate toxicity in rat motor cortex. PLoS One 26 78 PMID: 17240155
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Literature in this Area
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Huntington's Disease Poster
Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.