Drug intelligence / Profile preview

ML297

Development stage
Preclinical
Lead developer
Vanderbilt University
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

ML297 (also known as VU0456810) is a potent, selective, and brain-penetrant small molecule activator of G-protein-gated inwardly rectifying potassium (GIRK) channels, specifically targeting GIRK1-containing heterotetramers (such as GIRK1/2, GIRK1/3, and GIRK1/4). Developed by researchers at Vanderbilt University, ML297 serves as a valuable chemical probe to investigate the physiological and therapeutic roles of GIRK channels. In preclinical studies, ML297 has demonstrated significant efficacy in animal models of epilepsy and anxiety, reducing seizure activity and anxiety-related behaviors without causing sedation or addictive effects. Additionally, it has been studied in vitro for its effects on pre-osteoblast cell proliferation.

Other names
1-(3,4-difluorophenyl)-3-(3-methyl-1-phenyl-1H-pyrazol-5-yl)ureaN-(3,4-difluorophenyl)-N'-(3-methyl-1-phenyl-1H-pyrazol-5-yl)urea
02

Targets

KCNJ3 (GIRK1)KCNJ6 (G protein-activated inward rectifier potassium channel 2)

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