Taspoglutide is a pharmaceutical drug, a glucagon-like peptide-1 agonist (GLP-1 agonist), under investigation for treatment of type 2 diabetes being codeveloped by Ipsen and Roche.
CAT No: 10-101-176
CAS No:275371-94-3
Synonyms/Alias:275371-94-3;SCHEMBL2899791;Taspoglutide trifluoroacetate salt;DB14027;DA-67943;ITM077; R1583; BIM51077;F85503;
Taspoglutide is a synthetic peptide analog of glucagon-like peptide-1 (GLP-1), designed to mimic the activity of endogenous incretin hormones involved in glucose metabolism. As a stabilized GLP-1 receptor agonist, it features specific amino acid substitutions that enhance its resistance to enzymatic degradation, thereby prolonging its biological activity. Taspoglutide's unique peptide structure and receptor selectivity have made it a valuable tool in biochemical and pharmacological research focused on metabolic regulation, signal transduction, and peptide-based therapeutic mechanisms. Its well-characterized action on GLP-1 receptors enables detailed exploration of peptide hormone function, receptor-ligand interactions, and downstream cellular effects relevant to metabolic homeostasis.
Receptor Pharmacology: In receptor binding and signaling studies, taspoglutide serves as a potent and selective agonist for the GLP-1 receptor. Researchers employ it to characterize receptor activation profiles, investigate ligand-induced conformational changes, and dissect the molecular mechanisms underlying peptide-receptor specificity. Its stability and receptor affinity make it particularly useful for in vitro assays that require sustained receptor engagement, facilitating detailed kinetic and structural analyses of GLP-1 receptor function.
Metabolic Pathway Research: Taspoglutide is frequently utilized to model incretin-mediated signaling cascades in cellular and animal systems. By activating GLP-1 receptors, it enables the study of downstream pathways such as cAMP production, insulinotropic signaling, and β-cell function. These investigations contribute to a deeper understanding of metabolic regulation, insulin secretion mechanisms, and the broader role of peptide hormones in energy homeostasis. The compound's resistance to dipeptidyl peptidase-4 (DPP-4) degradation allows for precise temporal control in experimental designs.
Peptide Drug Development: In the context of peptide engineering and drug discovery, taspoglutide acts as a reference molecule for the design and optimization of next-generation GLP-1 analogs. Its well-documented structure-activity relationships and pharmacokinetic properties provide a benchmark for evaluating novel peptide modifications aimed at improving receptor selectivity, bioavailability, or stability. Researchers leverage it to compare efficacy, receptor signaling bias, and degradation profiles among candidate molecules, accelerating the development of innovative peptide-based agents.
Analytical Method Development: The defined sequence and stability of taspoglutide make it an ideal standard in the development and validation of analytical techniques for peptide quantification. It is commonly used in high-performance liquid chromatography (HPLC), mass spectrometry, and immunoassay calibration to ensure accurate detection and measurement of GLP-1 analogs in complex biological matrices. Its application in analytical workflows supports method robustness, reproducibility, and sensitivity in peptide analysis.
Structure-Function Studies: Taspoglutide's engineered amino acid substitutions provide a model for investigating the impact of sequence modifications on peptide conformation, receptor interaction, and biological function. Structural biologists and biochemists use it to elucidate the relationship between peptide design and functional outcomes, employing techniques such as X-ray crystallography, NMR spectroscopy, and molecular dynamics simulations. These studies advance the understanding of peptide-based ligand design and inform the rational development of new bioactive peptides with tailored properties.
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