Drug intelligence / Profile preview

GT729 (The Wistar Institute)

Development stage
Preclinical
Lead developer
Grit Biotechnology
Modality
Small Molecules
Administration
Oral
01

Overview

GT729 is a small molecule negative allosteric modulator (NAM) of the Excitatory Amino Acid Transporter 2 (EAAT2), also known as SLC1A2. Developed by The Wistar Institute, it was identified through structure-activity relationship (SAR) studies aimed at creating modulators for the primary glutamate transporter in the central nervous system. The compound features a quinoline-2-one ring structure with methyl groups at positions 6 and 8, and an N-capped piperazine with a furanamide moiety. Unlike positive allosteric modulators that enhance glutamate clearance, GT729 modestly inhibits L-glutamate uptake. It is being investigated as a therapeutic candidate for central nervous system disorders characterized by glutamate dysregulation, including neurodegenerative diseases and epilepsy.

Other names
CAS 460328-20-5CAS460328-20-5CAS-460328-20-51-[4-(2-furoyl)piperazin-1-yl]-2-(6,8-dimethyl-2-oxoquinolin-1(2H)-yl)ethanone
02

Targets

SLC1A2 (Glutamate Transporter 1)

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