| Description | UCPH-101 is an inhibitor of excitatory amino acid transporter subtype 1 (EAAT1) with an IC50 of 0.66 μM. |
| In vitro | 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). 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. |
| Target activity | EAAT1:0.66 μM. |
| Synonyms | UCPH 101 |
| molecular weight | 422.48 |
| Molecular formula | C27H22N2O3 |
| CAS | 1118460-77-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10.6 mg/mL(25 mM) |
| References | 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. |