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, also known as AMG 416, is a synthetic peptide composed of seven D-amino acids, engineered to interact specifically with the calcium-sensing receptor (CaSR) on the surface of parathyroid cells. Its unique structure enables it to mimic the action of endogenous calcium, thereby modulating parathyroid hormone (PTH) secretion through allosteric activation of the receptor. Etelcalcetide's high selectivity for CaSR, combined with its peptide backbone, makes it a valuable research tool for investigating calcium homeostasis and the molecular mechanisms underlying parathyroid function. The compound's stability in biological matrices and its capacity for reversible receptor binding further enhance its utility in experimental systems, supporting a range of scientific inquiries related to mineral metabolism and endocrine regulation.
Calcium-Sensing Receptor Studies: As a potent CaSR agonist, Etelcalcetide is widely utilized in laboratory studies aimed at elucidating the signaling pathways and conformational changes associated with calcium-sensing receptor activation. Researchers employ the compound to probe the receptor's response to allosteric modulation, facilitating the mapping of downstream signaling cascades, including those involving phospholipase C and intracellular calcium mobilization. By applying Etelcalcetide to cultured parathyroid cells or engineered cell lines expressing CaSR, investigators can dissect the molecular determinants of receptor-ligand interactions and assess the effects of various mutations or pharmacological interventions on receptor function.
Parathyroid Hormone Regulation Research: AMG 416 serves as a critical tool in studies focused on the regulation of parathyroid hormone secretion and its broader implications for mineral metabolism. Its ability to suppress PTH release in vitro provides a controlled means of investigating the feedback loops governing calcium and phosphate balance. Scientists leverage Etelcalcetide in experimental models to explore the dynamics of PTH synthesis, secretion, and gene expression in response to CaSR activation, yielding insights into the physiological and pathophysiological processes that drive parathyroid gland activity.
Mineral Metabolism Investigations: The peptide's impact on calcium and phosphate homeostasis renders it valuable for research in the field of mineral metabolism. By modulating the activity of CaSR, Etelcalcetide enables researchers to study the interplay between calcium levels, PTH secretion, and downstream effects on bone and renal physiology. Experimental use of the compound in animal models or ex vivo tissue systems can clarify the mechanisms by which alterations in CaSR signaling contribute to disorders of mineral balance, such as those encountered in chronic kidney disease or secondary hyperparathyroidism.
Endocrine System Modeling: Etelcalcetide is also employed in the development of in vitro and in vivo models of endocrine regulation, particularly those involving the parathyroid gland and its hormonal outputs. The compound's predictable pharmacodynamic profile allows for the simulation of altered parathyroid activity, providing a platform for testing hypotheses related to endocrine feedback, receptor desensitization, and compensatory mechanisms within the hypothalamic-pituitary-parathyroid axis. Such models are instrumental in advancing the understanding of endocrine disorders and their systemic effects.
Structure-Activity Relationship (SAR) Analysis: The unique peptide structure of AMG 416 makes it an exemplary candidate for SAR studies aimed at optimizing CaSR-targeted ligands. Researchers utilize Etelcalcetide as a reference compound to compare the efficacy, potency, and receptor selectivity of novel analogs or modified peptides. By systematically varying amino acid sequences or chemical modifications, scientists can delineate the structural features critical for receptor engagement and functional activity, supporting the rational design of next-generation CaSR modulators for research applications.
Signal Transduction Pathway Elucidation: In addition to its direct effects on parathyroid hormone regulation, Etelcalcetide is instrumental in unraveling the broader signal transduction networks associated with CaSR activation. Experimental application of the peptide enables the characterization of intracellular pathways, such as MAPK and PI3K/Akt, that are engaged upon receptor stimulation. Through these studies, researchers gain a more comprehensive understanding of how calcium-sensing mechanisms integrate with cellular signaling processes, informing both basic science and translational research in endocrinology and cell biology.
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