UCPH-102 an analog of UCPH-101 and is a selective inhibitor of the glutamate transporter EAAT1 (excitatory amino acid transporter subtype 1) (IC50 = 0.42 µM and >300 µM at EAAT2-5). UCPH-102 is blood-brain barrier permeable (unlike UCPH-101) and active in vivo
Solubility & Handling
Storage instructions
-20°C
Solubility overview
Soluble in DMSO (25 mM)
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
Probing for improved potency and in vivo bioavailability of excitatory amino acid transporter subtype 1 inhibitors UCPH-101 and UCPH-102: design, synthesis and pharmacological evaluation of substituted 7-biphenyl analogs.
Erichsen et al (2014) Neurochem Res 39(10) : 1964-79
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 et al (2013) J Neurosci 33(3) : 1068-87