Drug intelligence / Profile preview

methyl 4-(2,3-dihydroxy-5-methylphenoxy)-2-hydroxy-6-methylbenzoate

Development stage
Preclinical
Lead developer
University of Chicago
Modality
Small Molecules
01

Overview

Methyl 4-(2,3-dihydroxy-5-methylphenoxy)-2-hydroxy-6-methylbenzoate, also known by code names such as MeGFN and Methyl Gerfelin, is a small molecule identified as a pharmacological inhibitor of Lactoylglutathione Lyase (GLO1). GLO1 is an enzyme responsible for detoxifying methylglyoxal (MG), a glycolytic byproduct. By inhibiting GLO1, this compound leads to an increase in MG levels, which acts as a competitive partial agonist at GABA-A receptors. This mechanism has shown potential in preclinical studies as a fast-acting antidepressant, reducing immobility in various antidepressant assay models. Research into this compound has been conducted by academic institutions including the University of Chicago, University of California San Diego, and University of Wisconsin-Milwaukee.

Other names
Methyl GerfelinGerfelin methylMethylgerfelinmethyl-gerfelinGerfelin methyl esterJWQ46YJR3QJWQ-46YJR3QJWQ 46YJR3QRefChem:815825700870-56-02za0orb1983383orb-1983383orb 1983383SCHEMBL23752499SCHEMBL-23752499SCHEMBL 23752499DTXSID40220361DTXSID-40220361DTXSID 40220361BDBM50517464BDBM-50517464BDBM 50517464Q27097408Q-27097408Q 27097408Methyl 4-(2,3-dihydroxy-5-methylphenoxy)-6-hydroxy-2-methylbenzoateBenzoic acid, 4-(2,3-dihydroxy-5-methylphenoxy)-2-hydroxy-6-methyl-, methyl ester
02

Targets

GLO1 (Glyoxalase 1)

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