UCPH 101

(HB0630)

Product overview

  • Name
    UCPH 101
  • Short description
    UCPH-101 is a potent, selective, non-competitive EAAT1 inhibitor
  • Biological description

    UCPH-101 is a potent, selective, non-competitive inhibitor of the EAAT1 (Excitatory Amino Acid Transporter 1) glutamate transporter (IC50 = 660 nM). UCPH-101 shows >400-fold selectivity for EAAT1 over EAAT2 and EAAT3 and shows no inhibitory activity at EAAT4 and EAAT5 in a patch-clamp electrophysiology assay (in which final concentration was up to 10 μM). UCPH-102 which is blood brain barrier permeable is now also available.

  • Biological action
    Inhibitor
  • Purity
    >98%
  • Citations

Properties

  • Chemical name
    2-Amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-4H-chromene- 3-carbonitrile
  • Molecular Weight
    422.48
  • Chemical structure
    UCPH 101  [1118460-77-7]
  • Molecular Formula
    C27H22N2O3
  • CAS Number
    1118460-77-7
  • PubChem identifier
    25223366
  • SMILES
    COC1=CC=C(C=C1)C2C(=C(OC3=C2C(=O)CC(C3)C4=CC=CC5=CC=CC=C54)N)C#N
  • Source
    Synthetic
  • InChi
    InChI=1S/C27H22N2O3/c1-31-19-11-9-17(10-12-19)25-22(15-28)27(29)32-24-14-18(13-23(30)26(24)25)21-8-4-6-16-5-2-3-7-20(16)21/h2-12,18,25H,13-14,29H2,1H3
  • InChiKey
    YBMGNDPBARCLFT-UHFFFAOYSA-N
  • Appearance
    White solid

Storing and Using Your Product

  • Storage instructions
    +4°C
  • Solubility overview
    Soluble in DMSO (25mM)
  • Important
    This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

References for UCPH 101

  • Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1.

    Jensen AA et al (2009) J Med Chem 52(4) : 912-5.
    PubMedID: 19161278
  • Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102.

    Huynh TH et al (2012) Bioorg Med Chem 20(23) : 6831-9.
    PubMedID: 23072958
  • 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 B et al (2013) J Neurosci 33(3) : 1068-87.
    PubMedID: 23325245

Reviews & Product Guides