Etelcalcetide, also known as AMG 416 and KAI-4169, is a D-amino peptide calcimimetic undergoing clinical evaluation for the treatment of secondary hyperparathyroidism for patients with chronic kidney disease (CKD) on hemodialysis. Etelcalcetide is administered intravenously at the end of each dialysis session. It functions by binding to and activating the calcium-sensing receptor (CaSR) in the parathyroid gland as an allosteric activator, resulting in PTH reduction and suppression. Elevated PTH is often observe in patients with CKD.
CAT No: R1962
CAS No:1334237-71-6
Synonyms/Alias:etelcalcetide hydrochloride;1334237-71-6;etelcalcetide HCl;Velcalcetide Hydrochloride;KAI-4169 HCl;Telcalcetide hydrochloride;UNII-72PT5993DU;AMG 416;72PT5993DU;Etelcalcetide hydrochloride [USAN];KAI-4169 hydrochloride;N-Acetyl-D-cysteinyl-D-alanyl-D-arginyl-D-arginyl-D-arginyl-D-alanyl-D-argininamide disulfide with L-cysteine hydrochloride;D-ARGININAMIDE, N-ACETYL-D-CYSTEINYL-D-ALANYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ALANYL-, DISULFIDE WITH L-CYSTEINE, HYDROCHLORIDE;CHEMBL3545183;SCHEMBL22578458;DTXSID70158103;EX-A7480;ETELCALCETIDE HYDROCHLORIDE [MI];ETELCALCETIDE HYDROCHLORIDE [JAN];BE165527;ETELCALCETIDE HYDROCHLORIDE [WHO-DD];G16652;AMG 416 hydrochloride; KAI-4169 hydrochloride;Q27266087;AMG-416, AMG416, AMG 416, KAI-4169, KAI 4169, KAI4169, ONO5163, ONO-5163, ONO 5163, Etelcalcetide, Velcalcetide, Telcalcetide. Ac-D-Cys-D-Ala-D-Arg-D-Arg-D-Arg-D-Ala-D-Arg-NH2.Etelcalcetide HCl.;D-Argininamide, N-acetyl-D-cysteinyl-D-alanyl-D-arginyl-D-arginyl-D-arginyl-D-alanyl-, disulfide with L-cysteine, hydrochloride (1:?);
Chemical Name:(2R)-3-[[(2S)-2-acetamido-3-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-oxopropyl]disulfanyl]-2-aminopropanoic acid;hydrochloride
Etelcalcetide Hydrochloride is a synthetic peptide compound that functions as a calcium-sensing receptor (CaSR) agonist, specifically designed to modulate extracellular calcium homeostasis. Structurally, it consists of a linear chain of amino acids with a unique configuration that enables it to interact selectively with the CaSR, a critical G protein-coupled receptor involved in the regulation of parathyroid hormone (PTH) secretion. As a tool compound in biochemical research, Etelcalcetide Hydrochloride offers valuable opportunities for investigating calcium signaling pathways, receptor pharmacology, and peptide-receptor interactions. Its well-characterized mechanism of action and high receptor specificity make it a versatile agent for both fundamental and applied research in endocrinology, pharmacology, and peptide science.
Receptor Pharmacology: Etelcalcetide Hydrochloride is widely utilized in studies focused on the pharmacological characterization of the calcium-sensing receptor. By serving as a potent agonist, it enables researchers to probe CaSR activation dynamics, ligand-receptor binding affinities, and downstream signaling cascades. Its application in in vitro assays facilitates the dissection of receptor-mediated pathways, allowing for the elucidation of molecular mechanisms underlying calcium-regulated cellular processes. This peptide is especially valuable in the context of receptor mutagenesis studies, where it helps define the structural determinants of ligand recognition and receptor activation.
Calcium Homeostasis Research: The compound is instrumental in experimental models investigating systemic and cellular calcium regulation. By modulating CaSR activity, Etelcalcetide Hydrochloride provides a means to simulate altered extracellular calcium conditions and study their effects on parathyroid hormone release, intracellular signaling, and related metabolic processes. Such research is fundamental for understanding the physiological and pathophysiological roles of calcium-sensing mechanisms in various tissues, including the parathyroid gland, kidneys, and bone.
Peptide-Receptor Interaction Studies: As a synthetic peptide with a defined sequence and mode of action, Etelcalcetide Hydrochloride is an excellent model for exploring peptide-receptor interactions. It enables detailed biophysical and structural analyses, including binding kinetics, conformational changes upon receptor engagement, and the identification of critical contact residues. These studies contribute to the broader field of peptide drug discovery by informing the rational design of new receptor-targeted molecules with improved specificity and efficacy.
Signal Transduction Pathway Analysis: The ability of Etelcalcetide Hydrochloride to selectively activate the CaSR makes it a valuable probe for dissecting intracellular signaling networks downstream of receptor engagement. Researchers use it to map the activation of G protein-dependent and independent pathways, measure second messenger production, and assess the modulation of gene expression profiles. These insights are crucial for understanding how extracellular calcium fluctuations translate into specific cellular responses and for identifying novel regulatory nodes within the calcium signaling axis.
Peptide Synthesis and Analytical Method Development: Etelcalcetide Hydrochloride's defined structure and receptor selectivity render it useful as a reference standard in peptide synthesis optimization and analytical method validation. It is employed to calibrate chromatographic and mass spectrometric techniques, assess peptide purity, and establish assay sensitivity for similar peptide-based compounds. Its utility in these technical applications supports the advancement of peptide manufacturing processes and quality control methodologies within the biochemical industry.
Collectively, Etelcalcetide Hydrochloride serves as a multifaceted research tool, advancing scientific understanding of calcium-sensing receptor function, peptide-receptor pharmacology, and the broader landscape of calcium-mediated cellular regulation. Its applications span from basic mechanistic studies to the development of analytical protocols, underscoring its significance in both academic and industrial research settings.
If you have any peptide synthesis requirement in mind, please do not hesitate to contact us at . We will endeavor to provide highly satisfying products and services.
Creative Peptides is a trusted CDMO partner specializing in high-quality peptide synthesis, conjugation, and manufacturing under strict cGMP compliance. With advanced technology platforms and a team of experienced scientists, we deliver tailored peptide solutions to support drug discovery, clinical development, and cosmetic innovation worldwide.
From custom peptide synthesis to complex peptide-drug conjugates, we provide flexible, end-to-end services designed to accelerate timelines and ensure regulatory excellence. Our commitment to quality, reliability, and innovation has made us a preferred partner across the pharmaceutical, biotechnology, and personal care industries.
Read More