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 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1118460-77-7 |
| PubChem ID | 25223366 |
| InChI Key | YBMGNDPBARCLFT-UHFFFAOYSA-N |
| Smiles | NC2=C(C#N)C(C3=CC=C(OC)C=C3)C1=C(O2)CC(C4=C(C=CC=C5)C5=CC=C4)CC1=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.56 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 422.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.37 mL | 11.83 mL | 23.67 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.73 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.37 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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 PMID:
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
Keywords: UCPH 101, supplier, Selective, non-substrate, EAAT1, inhibitors, inhibits, excitatory, amino, acid, transporters, glutamate, monoamine, neurotransmitter, GLAST, UCPH101, Glutamate, Transporters, Glutamate, Transporters, Tocris Bioscience
