Exendin-4 (CAS: 141758-74-9)

Exendin-4, also known as exenatide, is a 39-amino-acid incretin mimetic peptide originally isolated from the Gila monster (Heloderma suspectum). It is a high-affinity GLP-1 receptor agonist that can increase intracellular cAMP, promote glucose-dependent insulin secretion, suppress glucagon release, and delay gastric emptying. As a glucagon-like peptide-1 analog with enhanced stability and prolonged half-life, the synthetic exendin-4 peptide is widely used to treat type 2 diabetes and obesity.

Exendin-4 has also been shown to support overall pancreatic function, β-cell proliferation, and neuroprotection. Therefore, the exenatide peptide is studied for treating additional GLP-1 receptor-related diseases.

Synthetized by JPT Peptide Technologies, a leader in Custom Peptide Synthesis services. For research use only, do not use in humans!

Exendin-4 (CAS: 141758-74-9) - Specifications

• Peptide sequence: H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2
• Amount: 1.0 mg net (AAA)
• Purity: >95% (HPLC-MS)
• Counterion: TFA
• Delivery Format: Freeze-dried in plastic vial
• MW (average): 4186.59
• Application(s): Diabetes research
• Condition(s)/Topic(s): Diabetes
• Standard Delivery Time: 2-5 days
• CAS: 141758-74-9
• SMILES: N[C@@H](CC1=CNC=N1)C(NCC(N[C@@H](CCC(O)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H]([C@H](O)C)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CCC(N)=O)C(N[C@H](C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(N[C@H](C(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC4=CNC5=C4C=CC=C5)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CC(N)=O)C(NCC(NCC(N6[C@H](C(N[C@@H](CO)C(N[C@@H](CO)C(NCC(N[C@@H](C)C(N7CCC[C@H]7C(N8CCC[C@H]8C(N9CCC[C@H]9C(N[C@@H](CO)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC6)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)=O)CCSC)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O

Exenatide Mechanism of Action

1. Core Mechanism
   • GLP-1 Receptor Binding: Exendin-4 peptide mimics the action of endogenous incretin hormones and acts as a high-affinity agonist of the glucagon-like peptide-1 receptor (GLP-1R, Kd = 136 pM). This G-protein coupled receptor is expressed in pancreatic β-cells and other tissues.
   • Activation of cAMP Signaling: Following receptor activation, the GLP-1 analog stimulates adenylate cyclase, increasing intracellular cAMP levels and initiating downstream signaling pathways such as PKA, Epac2, and CREB.
2. Primary Hypoglycemic Effects
   • Glucose-Dependent Insulin Secretion: Increased cAMP enhances glucose-dependent insulin secretion from pancreatic β-cells by modulating ion channels and promoting insulin vesicle exocytosis.
   • Suppression of Glucagon Release: In parallel, Exendin-4 peptide reduces inappropriately elevated glucagon secretion from pancreatic α-cells, contributing to decreased hepatic glucose production. Together, these effects support glycemic control.
   • Modulation of Gastric Emptying and Appetite: The exenatide peptide additionally slows gastric emptying and reduces food intake, supporting body weight regulation.
3. Additional Effects
   • β-Cell Proliferation and Pancreatic Function: Studies also show signs of β-cell proliferation and improved pancreatic function through exendin 4 regulated gene expression.
   • Extended Neuroprotective Effects: It is also suggested that through GLP-1 receptor signaling in the central nervous system, Exendin-4 peptide reduces neuroinflammation, protects against glutamate-induced neurotoxicity, and supports neuronal survival.

Exendin-4 Research Areas and Applications

The GLP-1 receptor agonist is widely used in metabolic and cell signaling research to support the development of novel therapeutics. It serves as a versatile tool in both in vitro and in vivo models, enabling the investigation of complex biological processes and disease mechanisms:

• Exendin-4 Diabetes Research: Investigation of insulin secretion and glucose homeostasis via GLP-1 receptor activation in pancreatic β-cells, including evaluation of exenatide peptide as a hypoglycemic agent (e.g., Exenatide for type 2 diabetes: Byetta®).
• Obesity and Weight Regulation Studies: Analysis of appetite control, satiety signaling, gastric emptying, and energy balance to treat obesity and support research on exenatide for weight loss.
• Drug Development and Screening: Evaluation and optimization of GLP-1 receptor agonists and analogs for improved efficacy, stability, and therapeutic performance.
• Neuroprotective Research: Exploration of GLP-1 receptor signaling in the central nervous system, including neuroprotective effects, neuroinflammation reduction, and applications in neurodegenerative diseases such as Parkinson’s and Alzheimer’s.
• Cell Signaling Studies: Study of exenatide’s mechanism of action, including cAMP production and receptor-mediated signaling mechanisms downstream of GLP-1 receptor activation.
• Cardiovascular Research: Assessment of cardioprotective effects, including regulation of blood pressure, arterial stiffness, and recovery following myocardial infarction.
• Renal and Liver Disease Research: Investigation of therapeutic potential in chronic kidney disease and non-alcoholic fatty liver disease (NAFLD), focusing on reducing inflammation, oxidative stress, and improving metabolic function.
• Biomarker and Target Validation: Support for identifying and validating GLP-1 receptor-related biomarkers and targets in translational and clinical research.
• Regenerative Medicine and Wound Healing: Study of tissue repair processes, including angiogenesis and cell proliferation, particularly in diabetic wound healing models.
• Oncological Research: Investigation of potential anti-proliferative effects in exendin-4 cancer models through modulation of GLP-1-related signaling pathways.

Key Advantages of Exendin-4 Peptide

• High GLP-1 Receptor Specificity: Enables precise activation of GLP-1 receptor-mediated pathways for targeted analysis of metabolic and signaling processes.
• Enhanced Stability and Prolonged Half-life: Resistant to degradation by dipeptidyl peptidase-4 (DPP-4), resulting in a prolonged half-life compared to native GLP-1.
• Potent Biological Activity: Induces strong insulin secretion and robust downstream signaling responses in GLP-1 receptor-expressing cells.
• Versatile Use: Suitable for a wide range of experimental setups (in vitro and in vivo models).
• Well-Characterized and Reproducible: Demonstrates consistent and reliable effects across metabolic and cell signaling studies.

Why Choose JPT for Exenatide Peptide?

JPT Peptide Technologies has substantial, 20 years of expertise in providing millions of peptides in all formats, scales and modifications to the global scientific community. All our catalog peptides are provided with HPLC-MS analyses to confirm the identity and demonstrate the high quality of our peptides.

• High-throughput peptide synthesis for efficient and scalable production
• Manufactured in Germany under high quality standards
• Flexible ordering options, including bulk quantities and variable purities
• Freeze-dried aliquots available for enhanced stability and storage
• Proven expertise and dedicated support
• Cost-effective and scalable solutions tailored to your needs
• Extensive modification options through Custom Peptide Synthesis services!

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