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1118460-77-7

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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.

1118460-77-7SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 18, 2017

Revision Date: Aug 18, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-amino-4-(4-methoxyphenyl)-7-naphthalen-1-yl-5-oxo-4,6,7,8-tetrahydrochromene-3-carbonitrile

1.2 Other means of identification

Product number -
Other names UCPH 101

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1118460-77-7 SDS

1118460-77-7Downstream Products

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.

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