| Bioactivity | UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM. | ||||||||||||
| Target | IC50: 0.66 μM (EAAT1) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | UCPH-101 | ||||||||||||
| CAS | 1118460-77-7 | ||||||||||||
| Formula | C27H22N2O3 | ||||||||||||
| Molar Mass | 422.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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):106 |