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UCPH-102

Names

[ CAS No. ]:
1229591-56-3

[ Name ]:
UCPH-102

[Synonym ]:
4H-1-Benzopyran-3-carbonitrile, 2-amino-5,6,7,8-tetrahydro-4-methyl-7-(1-naphthalenyl)-5-oxo-
2-Amino-4-methyl-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile
UCPH-102
2-Amino-4-methyl-7-(1-naphthyl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile
2-Amino-5,6,7,8-tetrahydro-4-methyl-7-(1-naphthalenyl)-5-oxo-4H-1-benzopyran-3-carbonitrile

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others
Research Areas >> Neurological Disease

[Target]

IC50: 0.43 µM (EAAT1)[1].


[References]

[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):1068-87.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
610.7±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H18N2O2

[ Molecular Weight ]:
330.380

[ Flash Point ]:
323.2±31.5 °C

[ Exact Mass ]:
330.136841

[ LogP ]:
2.68

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.676

Related Compounds