For research use only. Not for therapeutic Use.
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder[1][2][3][4].
| Catalog Number | I037794 |
| CAS Number | 1229591-56-3 |
| Synonyms | 2-amino-4-methyl-7-naphthalen-1-yl-5-oxo-4,6,7,8-tetrahydrochromene-3-carbonitrile |
| Molecular Formula | C21H18N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H18N2O2/c1-12-17(11-22)21(23)25-19-10-14(9-18(24)20(12)19)16-8-4-6-13-5-2-3-7-15(13)16/h2-8,12,14H,9-10,23H2,1H3 |
| InChIKey | XZQMHUGTNOOYFX-UHFFFAOYSA-N |
| SMILES | CC1C(=C(OC2=C1C(=O)CC(C2)C3=CC=CC4=CC=CC=C43)N)C#N |
| Reference | [1]. Huynh TH, et al. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg Med Chem. 2012 Dec 1;20(23):6831-9. [2]. Haym I, et al. Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102. ChemMedChem. 2016 Feb 17;11(4):403-19. [3]. Stanulović V S, et al. Proliferation and Survival of T-cell Acute Lymphoblastic Leukaemia Depends on mTOR-regulated Glutamine Uptake and EAAT1-dependent Conversion of Glutamine to Aspartate and Nucleotides. bioRxiv. 2020. [4]. Abrahamsen B, et al. 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. 2013 Jan 16;33(3):1068-87. |
