GLP-3R is a triple hormone receptor agonist targeting the glucose-dependent insulinotropic polypeptide receptor (GIPR), glucagon receptor (GCGR), and glucagon-like peptide-1 receptor (GLP-1R), with a molecular weight of approximately 4,731 Da. This synthetic 39-amino acid peptide incorporates structural modifications designed to enhance metabolic stability and extend circulation time, including an Aib substitution at position 2 for resistance to dipeptidyl peptidase-IV (DPP-IV) degradation and a fatty acid moiety that promotes reversible albumin binding.
Retatrutide represents a next-generation incretin-based research peptide that combines the insulinotropic and appetite-regulating effects of GLP-1R and GIPR activation with glucagon receptor-mediated effects on energy expenditure and metabolic regulation. This unique triple agonist profile has made GLP-3R a valuable tool for investigating integrated metabolic signaling pathways and receptor co-activation mechanisms.
In GIPR-expressing cellular models, GLP-3R functions as a potent agonist of Gs-coupled signaling pathways, resulting in increased intracellular cAMP production and downstream activation of protein kinase A (PKA). In GLP-1R-expressing systems, GLP-3R demonstrates robust receptor activation with downstream effects on cAMP signaling, receptor trafficking, and transcriptional regulation. Activation of the glucagon receptor has been associated with modulation of hepatic glucose metabolism, lipid oxidation pathways, and cellular energy utilization mechanisms.
Pancreatic islet research applications include studies in β-cell lines and isolated islet preparations, where GLP-3R has been investigated for its effects on glucose-dependent insulin secretion, β-cell signaling dynamics, and receptor cross-talk mechanisms. In α-cell models, triple receptor activation has been examined for its influence on glucagon secretion and endocrine regulatory pathways.
Metabolic research applications include investigation of adipocyte function, lipid metabolism, mitochondrial activity, and thermogenic gene expression. Studies utilizing white and brown adipocyte cultures have explored the coordinated effects of GIPR, GLP-1R, and GCGR activation on energy balance, adipokine secretion, and substrate utilization.
Neuroscience research has examined Retatrutide in hypothalamic and brainstem neuronal models involved in appetite regulation, reward processing, and energy homeostasis. Triple receptor engagement has been associated with distinct transcriptional signatures and signaling profiles compared to single- or dual-receptor agonists, making GLP-3R an important research tool for studying complex neuroendocrine pathways.
Cardiovascular and hepatic research applications include investigations into cellular metabolism, inflammatory signaling pathways, lipid handling, and tissue-specific responses to incretin and glucagon receptor co-activation. GLP-3R continues to be studied across multiple preclinical models to better understand the physiological consequences of simultaneous GIPR, GLP-1R, and GCGR stimulation.
Erosyn Labs provides Retatrutide as a lyophilized powder at ≥98% purity as determined by HPLC, with identity confirmation by mass spectrometry. Available in 5 mg and 10 mg research quantities, each lot is accompanied by a comprehensive Certificate of Analysis. Reconstitution in bacteriostatic water is recommended. Store lyophilized material at -20°C, protected from light. Reconstituted solutions may be stored at 2–8°C for up to 30 days under aseptic laboratory conditions.
For research and laboratory use only. Not for human consumption.
