UCPH-101 | EAAT1 inhibitor

UCPH-101 (1118460-77-7) is a potent (IC₅₀ = 660 nM) and selective inhibitor of the excitatory amino acid transporter 1 (EAAT1).^1,2 It induced cell death in glioblastoma cells via intracellular glutamate accumulation. UCPH-101 also significantly increased survival in glioma-bearing mice.³

References/Citations
1) Jensen et al. (2009), Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1; J. Med. Chem., 52 912
2) Erichsen et al. (2010), Structure-Activity Relationship Study of the 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
3) Corbetta et al. (2019), Altered function of the glutamate-aspartate transporter GLAST, a potential therapeutic target in glioblastoma; Int. J. Cancer, 144 2539