UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 uM.
CAS：1118460-77-7
分子式：C27H22N2O3
分子量：422.48
纯度：98%
存储：Store at -20°C

Background:

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

UCPH-101 and UCPH-102 inhibit EAAT1 anion currents in a concentration-dependent manner, with KD values of 0.34±0.03 uM (Hill=1.3±0.13, n≥9) for UCPH-101 and 0.17±0.02 uM (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 uM UCPH-101 (p=0.048)[1].

参考文献:
[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.