[L-Ala2]-Etelcalcetide substitutes alanine at position 2, modifying steric constraints and backbone geometry. The peptide's thiol and disulfide characteristics remain central to its folding and interaction profile. Researchers investigate structural changes and reactivity patterns. Applications include analog comparison, impurity identification, and structure-function analysis.
CAT No: Z10-101-233
Synonyms/Alias:S-(((S)-2-acetamido-3-(((S)-1-(((R)-1-(((R)-1-(((R)-1-(((R)-1-(((R)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxopropan-2-yl)amino)-3-oxopropyl)thio)-L-cysteine; Etelcalcetide impurity 2; 2-L-Ala-Etelcalcetide
[L-Ala2]-Etelcalcetide is a specialized synthetic peptide derivative designed to modulate calcium-sensing receptor (CaSR) activity, making it a valuable research tool in the study of calcium homeostasis and related signaling pathways. Featuring a structural modification with the incorporation of two L-alanine residues, this compound exhibits distinct biochemical properties that differentiate it from native etelcalcetide. Its ability to interact selectively with CaSR provides researchers with a means to dissect complex signaling cascades associated with calcium regulation in various cellular environments. The unique molecular configuration of [L-Ala2]-Etelcalcetide not only enhances its stability but also contributes to its utility in advanced laboratory investigations, particularly in the context of peptide-receptor interactions and structure-activity relationship studies. As a result, this compound has become increasingly important in the toolkit of scientists seeking to unravel the mechanisms underlying calcium-mediated physiological and pathological processes.
Calcium-Sensing Receptor Research: [L-Ala2]-Etelcalcetide serves as a potent probe for exploring the functional dynamics of the calcium-sensing receptor. By selectively activating or modulating CaSR, it enables researchers to investigate downstream signaling events, gene expression changes, and cellular responses to altered extracellular calcium concentrations. The compound's distinctive structure allows for precise manipulation of receptor activity, facilitating the dissection of CaSR-mediated pathways in tissues such as the parathyroid gland, kidney, and bone. Through in vitro cellular assays and ex vivo tissue models, scientists can employ this peptide to gain insights into the physiological regulation of mineral ion balance and the molecular mechanisms that govern calcium signaling networks.
Signal Transduction Pathway Elucidation: In the realm of signal transduction research, [L-Ala2]-Etelcalcetide is instrumental for mapping the intricate cascades initiated by CaSR activation. By modulating receptor activity, it helps delineate the sequence of intracellular events, including the mobilization of second messengers, activation of kinases, and regulation of transcription factors. This peptide can be applied in a variety of biochemical and molecular biology assays to trace the propagation of signals from the cell surface to the nucleus, thereby advancing the understanding of how extracellular cues influence cellular function. The insights gained from such studies are vital for identifying potential targets for therapeutic intervention and for clarifying the role of aberrant CaSR signaling in disease states.
Peptide Engineering and Structure-Activity Relationship Studies: The modified sequence of [L-Ala2]-Etelcalcetide makes it an excellent candidate for structure-activity relationship (SAR) investigations. Researchers can utilize this compound as a reference molecule to compare the effects of specific amino acid substitutions on receptor binding affinity, efficacy, and selectivity. The insights derived from these comparative analyses inform the rational design of novel peptide ligands with improved pharmacological profiles. Furthermore, the peptide's stability and bioactivity render it suitable for advanced analytical techniques such as nuclear magnetic resonance (NMR) spectroscopy and X-ray crystallography, which are essential for elucidating the structural basis of peptide-receptor interactions.
Pharmacological Screening and Drug Discovery: [L-Ala2]-Etelcalcetide is frequently employed in pharmacological screening assays aimed at identifying new modulators of the CaSR. Its well-characterized activity profile makes it a reliable positive control or reference standard in high-throughput screening platforms. By benchmarking the effects of novel compounds against this peptide, researchers can efficiently evaluate the potency and specificity of candidate molecules. The compound's utility extends to the validation of assay systems and the optimization of lead compounds in early-stage drug discovery, ultimately accelerating the identification of promising agents for further investigation.
Cellular Physiology and Pathophysiology Models: In studies of cellular physiology and pathophysiology, [L-Ala2]-Etelcalcetide is used to model the impact of altered CaSR activity on cell function and tissue homeostasis. Through controlled application in cultured cell lines, organoids, or animal-derived tissues, it enables the assessment of changes in cellular proliferation, differentiation, apoptosis, and metabolic activity in response to calcium signaling modulation. These experimental models are essential for understanding how dysregulation of the CaSR contributes to pathophysiological conditions such as mineral ion imbalance and tissue remodeling. By leveraging the unique properties of this peptide, researchers can develop more accurate and informative models of disease mechanisms, paving the way for targeted interventions in calcium-related disorders.
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