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GLP-1 Receptor Agonists Explained

2026-01-28 10 min read

Glucagon-like peptide-1 (GLP-1) receptor agonists are one of the most-discussed peptide classes in the metabolic research community. The field has moved from single-receptor analogues to dual- and now triple-agonists. Here's how the receptor science evolved.

The GLP-1 axis

GLP-1 is an incretin hormone released by intestinal L-cells after a meal. It binds the GLP-1 receptor on pancreatic β-cells (driving glucose-dependent insulin secretion), and the GLP-1 receptor in the central nervous system (driving satiety signalling in pre-clinical models). Synthetic GLP-1 analogues are engineered to resist DPP-4 degradation, extending their half-life from minutes to days.

Single-receptor: GLP-1 class

Our GLP-1 class is a long-acting GLP-1 analogue with two key modifications: an Aib substitution at position 8 (DPP-4 resistance) and a fatty-acid moiety at position 26 (albumin binding for extended half-life). Once-weekly protocols are standard in the research literature.

Dual-receptor: GLP-2 class

The GLP-2 class engages both the GLP-1 and GIP (glucose-dependent insulinotropic polypeptide) receptors. The hypothesis: GIP co-activation amplifies the metabolic effects observed with single-receptor GLP-1 analogues while partially offsetting some GI side-effect signalling in pre-clinical models.

Triple-receptor: GLP-3 class

The GLP-3 class adds a third receptor — glucagon — to the agonist portfolio. Glucagon receptor activity boosts energy expenditure (thermogenesis in pre-clinical models), which complements the activity profile of GLP-1 and GIP. Early-stage research data suggest the largest effect magnitudes of any receptor-agonist class to date.

Beyond metabolic research

GLP-1 receptors are expressed widely beyond the pancreas, and researchers are also exploring the class in cardiovascular, neurodegenerative and inflammatory disease models.

Comparing in our catalog

ClassReceptorsCatalog page
SingleGLP-1GLP-1
DualGLP-1 + GIPGLP-2
TripleGLP-1 + GIP + GlucagonGLP-3

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