Cat. No. 3490
Chemical Name: 2-Amino-5,6,7,8-tetrahydro-4-(4-met
Biological ActivitySelective 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).
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
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.
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.
Jensen et al (2009) Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J.Med.Chem. 52 912. PMID: 19161278.
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Citations are publications that use Tocris products. Selected citations for UCPH 101 include:
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.
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.
Do you know of a great paper that uses UCPH 101 from Tocris? If so please let us know.
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Keywords: UCPH 101, supplier, Selective, non-substrate, EAAT1, inhibitors, inhibits, excitatory, amino, acid, transporters, glutamate, monoamine, neurotransmitter, GLAST, UCPH101, Tocris Bioscience, Glutamate Transporter Inhibitor products