Catalog Number: 3490
Chemical Name: 2-Amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-4H-chromene-3-carbonitrile
Biological Activity
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
  • M.Wt:
    422.48
  • Formula:
    C27H22N2O3
  • Solubility:
    Soluble to 25 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    1118460-77-7
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.
Background References
  1. Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1.
    Jensen et al.
    J.Med.Chem., 2009;52:912
  2. 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).
    Erichsen et al.
    J.Med.Chem., 2010;53:7180
  3. 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.
    Abrahamsen et al.
    J.Neurosci., 2013;33:1068
  4. Excitatory amino acid transporters as potential drug targets.
    Bunch et al.
    Exp.Opin.Ther.Targets, 2009;13:719
Citations:

The citations listed below are publications that use Tocris products. Selected citations for UCPH 101 include:

3 Citations: Showing 1 - 3
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  1. Differential regulation of glutamate transporter subtypes by pro-inflammatory cytokine TNF-α in cortical astrocytes from a rat model of amyotrophic lateral sclerosis.
    Authors: Dumont Et al.
    Stroke 2014;9:e97649
  2. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Vision Res 2014;171:5417
  3. Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses.
    Authors: Tse Et al.
    PLoS One 2014;103:49

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