UCPH-101 is a potent, selective, non-competitive inhibitor of the EAAT1 (Excitatory Amino Acid Transporter 1) glutamate transporter (IC50 = 660 nM). UCPH-101 shows >400-fold selectivity for EAAT1 over EAAT2 and EAAT3 and shows no inhibitory activity at EAAT4 and EAAT5 in a patch-clamp electrophysiology assay (in which final concentration was up to 10 μM). UCPH-102 which is blood brain barrier permeable is now also available.
Solubility & Handling
Storage instructions
+4°C
Solubility overview
Soluble in DMSO (25mM)
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
References are publications that support the biological activity of the product
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.
Abrahamsen B et al (2013) J Neurosci 33(3) : 1068-87.