UCPH-101

UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

IC50: 0.66 μM (EAAT1)[1]

UCPH-101 and UCPH-102 inhibit EAAT1 anion currents in a concentration-dependent manner, with KD values of 0.34±0.03 μM (Hill=1.3±0.13, n≥9) for UCPH-101 and 0.17±0.02 μM (Hill=0.97±0.11, n≥7) for UCPH-102. A small but significant decrease in the total expression levels of both HA-EAAT1 and HA-GLAST is observed in cells preincubated with 100 μM UCPH-101 (p=0.048)[1].

Cells are split into poly-D-lysine-coated black 96-well plates with clear bottom. At 16 to 24 h later, the medium is aspirated, and the cells are washed with 100 μL Krebs buffer [140 mM NaCl/4.7 mM KCl/2.5 mM CaCl2/1.2 mM MgCl2/11 mM HEPES/10 mM D-glucose, pH 7.4]; 50 μL Krebs buffer supplemented with various concentrations of UCPH-101 or TBOA is added to the wells, after which an additional 50 μL Krebs buffer supplemented with the FMP assay dye (1 mg/mL) is added to each well. The plate is incubated at 37°C in a humidified 5% CO2 incubator for 30 min and assayed in a reader measuring emission at 560 nm caused by excitation at 530 nm before and up to 1 min after addition of 33 μL Glu solution[1].

[1]. 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.

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