Etelcalcetide HCl

Product NameEtelcalcetide HCl
CAS1334237-71-6
MFC38H74ClN21O10S2
MW1084.71186
EINECS
MOL File1334237-71-6.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO:10.0(Max Conc. mg/mL);8.37(Max Conc. mM) PBS (pH 7.2):10.0(Max Conc. mg/mL);8.37(Max Conc. mM) Water:50.0(Max Conc. mg/mL);41.87(Max Conc. mM)
form	A crystalline solid
color	White to off-white
Sequence	Ac-d-Cys(Cys)-d-Ala-d-Arg-d-Arg-d-Arg-d-Ala-d-Arg-NH2 (Disulfide bridge: Cys-Cys)
InChIKey	CRSDUYHPKJMYMG-KZTORMJDNA-N

Usage And Synthesis

Uses

Etelcalcetide hydrochloride (AMG 416 hydrochloride; KAI-4169 hydrochloride) is a synthetic calcimimetic as an activator of the calcium sensing receptor (CaSR). Etelcalcetide hydrochloride is effective in lowering parathyroid hormone (PTH) concentrations in patients receiving dialysis with secondary hyperparathyroidism receiving hemodialysis, which is promising for research in the field of secondary hyperparathyroidism and chronic kidney disease[1][2].

in vivo

Etelcalcetide hydrochloride (2.5 μg/h and 20 μg/h, infusion, 3 days) significantly reduces plasma PTH concentrations and decreased the renal expression of Cyp24a1 with a higher delivery rate^[1].

Animal Model:	C57BL7/6J male mice
Dosage:	2.5 μg/h and 20 μg/h
Administration:	infusion, 3 days
Result:	Significantly reduced plasma PTH concentrations and unaltered Cldn14 expression with 2.5 μg/h, but decreased the renal expression of Cyp24a1 with 20 μg/h ^[1]

References

[1] Differential parathyroid and kidney Ca2+-sensing receptor activation in autosomal dominant hypocalcemia 1 DOI:10.1016/j.ebiom.2022.103947
[2] Fujioka A, et al. Effect of etelcalcetide on parathyroid hormone secretion by primary hyperparathyroidism patient-derived primary parathyroid cells[J]. J Bone Miner Metab. 2021 May;39(3):396-403. DOI:10.1007/s00774-020-01158-2