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Biological Activity for UCPH 101
UCPH 101 is a selective non-substrate inhibitor of EAAT1 (IC50 values are 660, >300000 and >300000 nM for EAAT1, EAAT2 and EAAT3 respectively). Also demonstrates no significant inhibition at EAAT4 or EAAT5 in a patch-clamp electrophysiology assay (at final concentration up to 10 μM).
Technical Data for UCPH 101
|Storage||Store at +4°C|
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 UCPH 101
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for UCPH 101
The following data is based on the product molecular weight 422.48. 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|
|0.25 mM||9.47 mL||47.34 mL||94.68 mL|
|1.25 mM||1.89 mL||9.47 mL||18.94 mL|
|2.5 mM||0.95 mL||4.73 mL||9.47 mL|
|12.5 mM||0.19 mL||0.95 mL||1.89 mL|
References for UCPH 101
References are publications that support the biological activity of the product.
Jensen et al (2009) Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J.Med.Chem. 52 912 PMID: 19161278
Erichsen et al (2010) Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101). J.Med.Chem. 53 7180 PMID: 20857912
Bunch et al (2009) Excitatory amino acid transporters as potential drug targets. Exp.Opin.Ther.Targets 13 719
Abrahamsen et al (2013) Allosteric modulation of an excitatory amino acid transporter: The subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J.Neurosci. 33 1068 PMID: 23325245
If you know of a relevant reference for UCPH 101, please let us know.
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Keywords: UCPH 101, UCPH 101 supplier, Selective, non-substrate, EAAT1, inhibitors, inhibits, excitatory, amino, acid, transporters, glutamate, monoamine, neurotransmitter, GLAST, UCPH101, Glutamate, Transporters, 3490, Tocris Bioscience
4 Citations for UCPH 101
Citations are publications that use Tocris products. Selected citations for UCPH 101 include:
Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Vision Res 171 5417 PMID: 25052197
Tse et al (2014) Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses. PLoS One 103 49 PMID: 25152321
Dumont et al (2014) Differential regulation of glutamate transporter subtypes by pro-inflammatory cytokine TNF-α in cortical astrocytes from a rat model of amyotrophic lateral sclerosis. Stroke 9 e97649 PMID: 24836816
Brancaccio et al (2017) Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling. Neuron 93 1420 PMID: 28285822
Do you know of a great paper that uses UCPH 101 from Tocris? Please let us know.
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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.