1229591-56-3

1229591-56-3 structure

Name: UCPH-102
Chemical Name: UCPH-102
CAS Number: 1229591-56-3
Molecular Formula: C₂₁H₁₈N₂O₂
Molecular Weight: 330.380
Catalog: Research Areas Cancer
Create Date: 2018-06-11 18:56:28
Modify Date: 2023-01-21 13:15:55
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].

Name	UCPH-102
Synonyms	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

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.