Description

Product Description

Exendin 4, Biotin Labeled is a chemically modified analog of Exendin 4 (HY-13443), a potent and selective glucagon-like peptide-1 receptor (GLP-1R) agonist. Derived from the natural exendin sequence found in the saliva of the Gila monster (Heloderma suspectum), this biotinylated version retains full receptor activity while incorporating a biotin moiety that allows easy conjugation to streptavidin-based detection systems.

This modification expands its versatility for use in receptor binding assays, ligand-receptor mapping, fluorescence imaging, and high-throughput screening (HTS) of GLP-1–targeted compounds. Researchers often utilize Exendin 4, Biotin Labeled to visualize and quantify GLP-1 receptor expression, study receptor internalization pathways, and monitor ligand-induced signaling events.

As a long-acting GLP-1 receptor agonist, Exendin 4 mimics the biological actions of endogenous GLP-1 but exhibits enhanced stability and prolonged receptor activation, due to its resistance to enzymatic degradation by dipeptidyl peptidase-4 (DPP-4). It plays a crucial role in the regulation of glucose metabolism, insulin secretion, appetite control, and β-cell survival.

The biotin labeling does not significantly alter its binding affinity or activity, allowing researchers to use it as a functional probe in receptor-ligand studies or in pull-down assays to isolate GLP-1R complexes. The peptide’s conjugation site is strategically placed away from the receptor-binding domain to maintain structural and biological integrity.

In experimental endocrinology, Exendin 4, Biotin Labeled serves as a valuable molecular tool to study type 2 diabetes, obesity, and energy metabolism, as well as intracellular signaling cascades such as cAMP generation, PKA activation, and ERK phosphorylation. Because of its high stability and specificity, it is also used in biosensor development, fluorescence resonance energy transfer (FRET) experiments, and surface plasmon resonance (SPR) assays for quantitative binding kinetics.

With ≥99% purity and precise chemical characterization, this reagent enables reproducible results in cell-based assays, receptor kinetics modeling, and molecular imaging. It supports the investigation of GLP-1 receptor distribution across tissues, helping researchers understand the receptor’s role in pancreatic β-cell function, neuronal circuits, and cardiovascular regulation.

Product Specifications

Mechanism of Action

Exendin 4, Biotin Labeled acts as a GLP-1 receptor agonist, engaging the class B G-protein–coupled receptor (GPCR) on pancreatic β-cells and other tissues. Upon receptor activation, the peptide stimulates the adenylate cyclase–cAMP–PKA signaling cascade, leading to enhanced glucose-stimulated insulin secretion (GSIS).

The peptide also promotes β-cell proliferation, inhibition of apoptosis, and delayed gastric emptying, collectively contributing to glucose homeostasis. While the biotin label does not alter the peptide’s ability to bind the receptor, it enables quantitative tracking of receptor engagement using streptavidin-based detection methods (e.g., ELISA, flow cytometry, and imaging).

Additionally, GLP-1 receptor activation by Exendin 4 enhances mitochondrial metabolism and ATP production, promoting efficient insulin release. It also modulates central appetite centers through hypothalamic signaling, contributing to reduced food intake and improved energy balance.

The biotin moiety provides a flexible handle for immobilization on biosensor surfaces, allowing kinetic measurements of ligand-receptor interactions through surface plasmon resonance (SPR) or bio-layer interferometry (BLI). This property makes the biotin-labeled version a preferred analytical probe for structure–activity relationship (SAR) studies of GLP-1 analogs.

Side Effects

As a research reagent, Exendin 4, Biotin Labeled is not intended for clinical or in vivo therapeutic use. While native Exendin 4 analogs can cause gastrointestinal symptoms such as nausea or decreased appetite in physiological studies, the biotin-labeled version is for in vitro or ex vivo research only, minimizing such risks.

Users should handle the compound under proper laboratory safety protocols—avoiding skin contact, inhalation, or ingestion. Stability and bioactivity should be preserved by avoiding repeated freeze–thaw cycles.

Disclaimer

All products are for laboratory research use only. Exendin 4, Biotin Labeled is not approved for human or animal therapeutic applications. Researchers are responsible for ensuring proper handling and disposal in accordance with institutional and regional safety guidelines.

Keywords

GLP-1 receptor agonist, biotin peptide, exendin analog, glucose metabolism research, receptor binding assay, streptavidin conjugate peptide, fluorescent peptide probe, diabetes research reagent, GLP-1 signaling peptide, metabolic peptide tool

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