Description

Product Description

Relsipatide (CAS 2843676-09-3), also known as BG128, is a synthetic peptide that functions as a dual receptor agonist for gastric inhibitory polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Both GIP and GLP-1 belong to the incretin hormone family, which plays a crucial role in postprandial glucose regulation, insulin secretion, and energy metabolism.

As a research-grade incretin mimetic, Relsipatide has emerged as a valuable molecular tool for exploring metabolic homeostasis, pancreatic β-cell physiology, and insulin sensitivity enhancement in preclinical studies. Its dual receptor activation mechanism differentiates it from traditional single-pathway incretin agents, allowing researchers to evaluate synergistic signaling and improved glucose-lowering effects.

Relsipatide exerts its biological activity by binding to GLP-1R and GIPR, both of which are G protein–coupled receptors (GPCRs) expressed on pancreatic β-cells, adipocytes, hepatocytes, and neuronal tissues. Upon receptor engagement, Relsipatide activates adenylyl cyclase, leading to elevated cyclic AMP (cAMP) levels and subsequent activation of protein kinase A (PKA) and Epac2 pathways. These signaling cascades facilitate glucose-stimulated insulin secretion (GSIS), β-cell proliferation, and enhanced mitochondrial metabolism.

In metabolic and obesity research, Relsipatide is instrumental for studying the incretin effect, energy expenditure, and body weight regulation. Dual incretin receptor activation has shown potential to improve insulin sensitivity, reduce hepatic steatosis, and modulate appetite signaling through hypothalamic control centers.

Relsipatide’s dual-target mechanism provides a unique platform for investigating next-generation antidiabetic strategies, including combined incretin therapies and metabolic modulators. It also enables comparative studies with GLP-1–only agonists such as Liraglutide, Semaglutide, and Dulaglutide, thereby elucidating the additive benefits of dual receptor pharmacology in glucose and lipid metabolism.

In cell-based assays and animal models, Relsipatide demonstrates strong receptor-binding affinity, enzyme resistance, and enhanced plasma stability, making it ideal for extended in vitro and in vivo experimentation. Researchers have reported that Relsipatide enhances β-cell survival under glucotoxic conditions, promotes adiponectin expression, and reduces inflammatory cytokine production, indicating broad metabolic benefits beyond insulin secretion.

Overall, Relsipatide serves as a powerful research peptide for elucidating incretin physiology, diabetic pathophysiology, and pharmacodynamic receptor interactions, providing valuable insights for drug discovery in metabolic disease research.

Product Specifications

Mechanism of Action

Relsipatide acts as a dual agonist of GIPR (Gastric Inhibitory Polypeptide Receptor) and GLP-1R (Glucagon-Like Peptide-1 Receptor), both of which are G protein–coupled receptors that regulate glucose metabolism.

Upon binding to these receptors, Relsipatide activates adenylyl cyclase, elevating intracellular cAMP levels. This leads to activation of PKA and Epac2, which in turn trigger exocytosis of insulin granules from pancreatic β-cells. The result is enhanced glucose-dependent insulin secretion, improved glucose tolerance, and reduced plasma glucose concentration in experimental systems.

Beyond insulinotropic effects, Relsipatide influences lipid metabolism and energy balance. GIPR activation promotes lipid storage regulation and adipocyte insulin sensitivity, while GLP-1R activation reduces gastric emptying, appetite, and food intake through central nervous system pathways.

Relsipatide’s dual action achieves a balanced metabolic modulation by combining GIP’s anabolic support with GLP-1’s catabolic and appetite-suppressing functions. This synergy makes it a potent tool for studying energy metabolism, obesity mechanisms, and insulin resistance.

Moreover, preclinical studies have demonstrated that Relsipatide enhances mitochondrial function, improves β-cell survival under oxidative stress, and reduces proinflammatory cytokine release. These multifaceted actions position it as an ideal peptide for studying incretin-based pharmacology and next-generation diabetes therapeutics.

Side Effects

In research environments, Relsipatide exhibits a low toxicity profile and a favorable safety margin. However, due to its potent incretin-mimetic activity, experimental overdosing may transiently affect glucose and lipid metabolism, leading to mild hypoglycemic responses in animal models.

Other potential laboratory-observed effects include mild gastrointestinal slowing, transient reduction in food intake, or metabolic adaptation due to incretin receptor overstimulation.

These effects are generally reversible and dose-dependent. No cytotoxicity or genotoxicity has been reported in in vitro studies. Relsipatide should be handled under appropriate research protocols and is not intended for clinical or therapeutic use.

Disclaimer

All data are provided for laboratory research use only. Relsipatide is not approved for human administration or clinical diagnosis.

Keywords

 CAS no 2843676-09-3, BG128, dual GIP GLP-1 agonist, incretin peptide, antidiabetic research, insulin secretion modulator, metabolic regulation, GLP-1 analog, GIP receptor activator

Shipping Guarantee

All shipments are handled under temperature-controlled logistics with vacuum-sealed and desiccated packaging to preserve peptide integrity. Each lot includes a Certificate of Analysis (COA) verifying ≥99% purity and mass spectrometry validation.

Trade Guarantee

Our production process adheres to GLP and ISO standards, ensuring reproducibility, traceability, and analytical transparency. We provide secure international shipping and quality assurance for every research batch.