1118460-77-7 Usage
Description
UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system. UCPH-1 is selective for EAAT1 over EAAT2 and EAAT3 with IC50 values of 0.66, >300, and >300 μM, respectively, in a radioligand uptake assay using HEK293 cells transfected with the human transporter. It selectively inhibits anion currents in tsA201 cells expressing human EAAT1 (Kd = 0.34 μM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 μM. UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier.
Uses
UCPH 101 is a subtype-selective inhibitor of human excitatory amino acid transporter subtype 1.
References
1) Jensen?et al.?(2009),?Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1; J. Med. Chem.,?52?912
2) Erichsen?et al.?(2010),?Structure-Activity Relationship Study of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1: 2-Amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101); J. Med. Chem.,?53?7180
3) Corbetta?et al.?(2019),?Altered function of the glutamate-aspartate transporter GLAST, a potential therapeutic target in glioblastoma; Int. J. Cancer,?144?2539
Check Digit Verification of cas no
The CAS Registry Mumber 1118460-77-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,1,8,4,6 and 0 respectively; the second part has 2 digits, 7 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1118460-77:
(9*1)+(8*1)+(7*1)+(6*8)+(5*4)+(4*6)+(3*0)+(2*7)+(1*7)=137
137 % 10 = 7
So 1118460-77-7 is a valid CAS Registry Number.
1118460-77-7Relevant articles and documents
Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1
Jensen, Anders A.,Erichsen, Mette N.,Nielsen, Christina W.,Stensb?l, Tine B.,Kehler, Jan,Bunch, Lennart
supporting information; experimental part, p. 912 - 915 (2009/12/25)
The discovery of the first class of subtype-selective inhibitors of the human excitatory amino acid transporter subtype 1 (EAAT1) and its rat orthologue GLAST is reported. An opening structure-activity relationship of 25 analogues is presented that addresses the influence of substitutions at the 4- and 7-positions of the parental skeleton 2-amino-5-oxo-5,6,7,8-tetrahydro-4H- chromene-3-carbonitrile. The most potent analogue 1o displays high nanomolar inhibitory activity at EAAT1 and a >400-fold selectivity over EAAT2 and EAAT3, making it a highly valuable pharmacological tool.