1229591-56-3

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].

UCPH-102 is a selective inhibitor of the Excitatory Amino Acid Transporter subtype-1 (EAAT1GLAST) with an IC50 value of 420 nM for EAAT1 and >300 μM for EAAT2-5. UCPH-102 has been shown to cross the blood-brain barrierso should become a valuable tool for studying the role of EAAT1 in brain.

EAAT1

[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. DOI:10.1016/j.bmc.2012.09.049
[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. DOI:10.1002/cmdc.201500527
[3] Stanulovi? 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. DOI:10.1523/JNEUROSCI.3396-12.2013