Etelcalcetide is used for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on hemodialysis. Etelcalcetide is a calcimimetic agent that allosterically modulates the calcium-sensing receptor (CaSR). Etelcalcetide binds to the CaSR and enhances activation of the receptor by extracellular calcium. Activation of the CaSR on parathyroid chief cells decreases PTH secretion.
CAT No: 10-101-140
CAS No:1262780-97-1
Synonyms/Alias:etelcalcetide;Velcalcetide;1262780-97-1;Parsabiv;AMG-416;KAI-4169;Telcalcetide;Etelcalcetida;AMG 416;UNII-60ME133FJB;60ME133FJB;KAI 4169;ONO-5163;Amg416;DTXSID70155132;D-Argininamide, N-acetyl-D-cysteinyl-D-alanyl-D-arginyl-D-arginyl-D-arginyl-D-alanyl-, disulfide with L-cysteine;N-ACETYL-D-CYSTEINYL-D-ALANYL-D-ARGINYL-D-ARGINYL-D-ARGINYL-D-ALANYL-D-ARGININAMIDE DISULFIDE WITH L-CYSTEINE;Etelcalcetide [USAN:INN];Etelcalcetidum;ETELCALCETIDE [MI];ETELCALCETIDE [INN];Etelcalcetide (USAN/INN);ETELCALCETIDE [USAN];ETELCALCETIDE [WHO-DD];GTPL8375;CHEMBL3545184;DTXCID2077623;SCHEMBL21982605;H05BX04;KAI4169;CHEBI:134700;BDBM627976;GLXC-10160;ETELCALCETIDE [ORANGE BOOK];HY-P1955;AKOS037648615;Etelcalcetide Hydrochloride(AMG-416);DB12865;CVD-0019441;BS-14875;DA-50394;DA-63291;FE162097;CS-0030931;NS00127425;D10676;D71178;EN300-25975978;Q21098973;(2R)-2-amino-3-{[(2S)-2-{[(1R)-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-4-carbamimidamido-1-{[(1R)-1-{[(1R)-4-carbamimidamido-1-carbamoylbutyl]carbamoyl}ethyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}butyl]carbamoyl}ethyl]carbamoyl}-2-acetamidoethyl]disulfanyl}propanoic acid;
Etelcalcetide is a synthetic peptide composed of seven D-amino acids, designed as a selective agonist of the calcium-sensing receptor (CaSR). As a peptide compound, it exhibits high specificity for CaSR, modulating calcium homeostasis through allosteric activation. Its unique disulfide-linked structure and peptide backbone make it a valuable tool for probing receptor-ligand interactions, receptor pharmacology, and downstream signaling pathways. Researchers in the fields of endocrinology, nephrology, and molecular pharmacology recognize its significance for elucidating the regulatory mechanisms governing calcium metabolism and parathyroid hormone (PTH) secretion.
Receptor pharmacology research: Etelcalcetide serves as a potent and selective modulator for studies involving the calcium-sensing receptor. Its peptide-based structure and mechanism of action enable researchers to investigate the conformational dynamics of CaSR, the intricacies of receptor activation, and the allosteric modulation of G protein-coupled receptors (GPCRs). By employing this compound in receptor binding assays or signal transduction studies, investigators can dissect the molecular determinants of CaSR activation and gain insight into structure-activity relationships that underlie receptor selectivity and efficacy.
Signal transduction analysis: As a tool compound, etelcalcetide is instrumental in dissecting intracellular signaling cascades initiated by CaSR activation. Researchers utilize it to examine downstream pathways such as phospholipase C activation, intracellular calcium flux, and MAPK signaling. Its application allows for the detailed mapping of the biochemical events that follow receptor engagement, facilitating the identification of potential regulatory nodes and cross-talk with other signaling systems. Such studies are essential for understanding how extracellular calcium levels are sensed and translated into cellular responses.
Peptide-receptor interaction studies: The unique disulfide-linked peptide structure of etelcalcetide provides a model system for exploring the principles of peptide-receptor recognition and binding affinity. Its use in structural biology, including NMR spectroscopy and crystallography, enables the elucidation of key contacts between peptide ligands and GPCRs. These insights inform the rational design of next-generation peptide modulators with improved pharmacological profiles and selectivity for CaSR or related receptors.
Peptide synthesis and analytical method development: Etelcalcetide offers a reference standard for optimizing peptide synthesis protocols, particularly those involving D-amino acid incorporation and disulfide bond formation. Its well-characterized sequence and structure make it suitable for validating chromatographic and spectrometric analytical methods. Researchers and technical teams employ it to benchmark synthetic efficiency, purity assessment, and stability studies, enhancing peptide manufacturing and quality control workflows.
Functional studies in calcium homeostasis: The compound is widely adopted in experimental models to probe the physiological consequences of CaSR activation on calcium and phosphate metabolism. By modulating receptor activity in ex vivo or in vitro systems, etelcalcetide enables the assessment of PTH secretion dynamics, cellular calcium handling, and feedback mechanisms within endocrine pathways. Such applications advance the understanding of mineral metabolism and support the development of research tools targeting calcium-sensing mechanisms in health and disease models.
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