Drug intelligence / Profile preview

ML-133

Development stage
Unknown
Lead developer
Vanderbilt Specialized Chemistry Center for Accelerated Probe Development
Modality
Small Molecules
Administration
Oral
01

Overview

ML-133 is a potent and selective small molecule inhibitor of the Kir2 family of inwardly rectifying potassium channels, specifically targeting Kir2.1, Kir2.2, Kir2.3, and Kir2.6. Discovered through a high-throughput screen of over 300,000 compounds by the Molecular Libraries Probe Production Centers Network (MLPCN), it exhibits an IC50 of 1.8 μM for Kir2.1 at physiological pH (7.4). The compound is highly selective for the Kir2.x subfamily, showing little to no activity against other Kir channels such as Kir1.1, Kir4.1, and Kir7.1. In preclinical animal models, ML-133 has demonstrated efficacy in preventing the development of dynamic mechanical allodynia associated with nerve injury, suggesting its utility as a pharmacological probe for investigating neuropathic pain and the physiological roles of Kir2 channels in excitable tissues. It is primarily utilized as a chemical research tool.

Other names
N-(4-methoxybenzyl)-1-(naphthalen-1-yl)methanamine hydrochlorideN-[(4-methoxyphenyl)methyl]-1-naphthalenemethanamine hydrochloride
02

Targets

KCNJ12 (Kir2.2)KCNJ18 (Inward rectifier potassium channel 18)KCNJ2 (Inward rectifier potassium channel Kir2.1)KCNJ4 (Inward rectifier potassium channel 2.3)

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