A noncompetitive inhibitor of EAAT1; selective for EAAT1 over EAAT2 and EAAT3 (IC50s = 0.66

UCPH-101 – 500 µg

Brand:
Cayman
CAS:
1118460-77-7
Storage:
-20
UN-No:
Non-Hazardous - /

UCPH-101 is a noncompetitive inhibitor of excitatory amino acid transporter 1 (EAAT1), which takes up extracellular glutamate in the central nervous system.{40197,40196} 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.{40198} 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.{40196} UCPH-101 is orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier.{40197}  

 

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Description

A noncompetitive inhibitor of EAAT1; selective for EAAT1 over EAAT2 and EAAT3 (IC50s = 0.66, >300, and >300 µM, respectively); selective for human EAAT1 (Kd = 0.34 µM) over rat EAAT4 and mouse EAAT5 at concentrations up to 10 µM in an electrophysiology study; orally bioavailable in rats at a dose of 10 mg/kg but does not cross the blood-brain barrier

Formal name: 2-amino-5,6,7,8-tetrahydro-4-(4-methoxyphenyl)-7-(1-naphthalenyl)-5-oxo-4H-1-benzopyran-3-carbonitrile

Synonyms: 

Molecular weight: 422.5

CAS: 1118460-77-7

Purity: ≥98% (mixture of isomers)

Formulation: A solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience

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