Product overview

Name UCPH 101
Purity >98%
Description UCPH-101 is a potent, selective, non-competitive EAAT1 inhibitor
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Biological Data

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.

Solubility & Handling

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.

Calculators

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Chemical Data

Purity >98%
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] Chemical Structure
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

References for UCPH 101

References are publications that support the biological activity of the product
  • 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.
  • 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.
  • 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.

3 Item(s)

Publications
These publications cite the use of UCPH 101 purchased from Hello Bio:
  • Complete but not partial inhibition of glutamate transporters exacerbates cortical excitability in the R6/2 mouse model of Huntington's disease.

    Estrada-Sánchez et al (2018) CNS Neurosci Ther doi: 10.1111/ : cns.13070.
    PubMedID: 30311425

1 Item