GLP-2 is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist with a molecular weight of approximately 4,813.45 Da. This 39-amino acid synthetic peptide is based on the native GIP sequence with incorporated modifications that confer dual receptor activity: an Aib substitution at position 2 for DPP-IV resistance and a C20 fatty diacid acylation at Lys20 via a linker for albumin binding. GLP-2 represents a novel class of dual incretin receptor agonists and has become a critical research tool for investigating the complementary and synergistic effects of GIP and GLP-1 receptor co-activation.
In GIPR-expressing cell models, GLP-2 demonstrates potent agonist activity, activating Gs-coupled cAMP/PKA signaling with efficacy comparable to native GIP. In GLP-1R-expressing cell lines, GLP-2 functions as an imbalanced agonist, exhibiting biased signaling characterized by robust cAMP generation with attenuated β-arrestin recruitment relative to native GLP-1. This biased agonism profile has been extensively characterized using BRET-based recruitment assays and is an area of active investigation in GPCR pharmacology.
Pancreatic islet research applications include studies in β-cell lines (INS-1, MIN6) and isolated islet preparations, where dual receptor activation by GLP-2 has demonstrated synergistic enhancement of glucose-dependent insulin secretion exceeding that of selective GLP-1R or GIPR agonists alone. In α-cell models, GLP-2 has been studied for effects on glucagon secretion dynamics. Adipocyte research has identified GIPR-mediated effects of GLP-2 on lipid storage, adiponectin expression, and thermogenic gene programs in brown and white adipocyte cultures.
Neuroscience applications include investigation of central GLP-1R and GIPR signaling in hypothalamic neuronal models, where dual receptor engagement has been associated with distinct transcriptional profiles compared to single-receptor agonism. Cardiovascular research has examined GLP-2 in cardiomyocyte and endothelial cell models for cardioprotective and anti-inflammatory signaling properties.
Erosyn Labs provides GLP-2 as a lyophilized powder at ≥98% purity by HPLC with mass spectrometry identity confirmation, available in 5 mg and 10 mg research quantities. A comprehensive Certificate of Analysis accompanies each lot. Reconstitution in bacteriostatic water is recommended. Store lyophilized material at -20°C, protected from light. Reconstituted solutions at 2–8°C for up to 30 days. Handle under aseptic conditions.
For research and laboratory use only. Not for human consumption.
