| Bioactivity | UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder[1][2][3][4]. |
| Target | IC50: 0.43 µM (EAAT1). |
| Name | UCPH-102 |
| CAS | 1229591-56-3 |
| Formula | C21H18N2O2 |
| Molar Mass | 330.38 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Huynh TH, et al. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg Med Chem. 2012 Dec 1;20(23):6831-9. [2]. Haym I, et al. Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102. ChemMedChem. 2016 Feb 17;11(4):403-19. [3]. Stanulović V S, et al. Proliferation and Survival of T-cell Acute Lymphoblastic Leukaemia Depends on mTOR-regulated Glutamine Uptake and EAAT1-dependent Conversion of Glutamine to Aspartate and Nucleotides. bioRxiv. 2020. [4]. 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 |