Drug intelligence / Profile preview

Metabolex-36

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral, Intperitoneal
01

Overview

Metabolex-36 is a selective small molecule agonist of the G protein-coupled receptor 120 (GPR120), also known as Free Fatty Acid Receptor 4 (FFAR4). Developed by CymaBay Therapeutics (formerly Metabolex), the compound was investigated as a potential treatment for type 2 diabetes. It demonstrates high potency with EC50 values of 570 nM for human GPR120 and 130 nM for mouse GPR120. Metabolex-36 is highly selective for FFAR4 and does not activate the related receptor GPR40 (FFAR1). Preclinical studies in animal models have shown that the compound improves oral glucose tolerance, enhances insulin secretion, and stimulates the release of glucagon-like peptide-1 (GLP-1) from enteroendocrine cells.

Other names
GPR120 agonist Compound HGPR-120 agonist Compound HGPR 120 agonist Compound H
02

Targets

FFAR4 (Free fatty acid receptor 4)FFAR1 (Free fatty acid receptor 1)

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