A peptide agonist of CaSR
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Etelcalcetide (hydrochloride)

Item No. 26901

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-acetyl-D-cysteinyl-D-alanyl-D-arginyl-D-arginyl-D-arginyl-D-alanyl-D-argininamide, disulfide with L-cysteine, hydrochloride
CAS Number
1334237-71-6
Synonyms
  • KAI 4169
  • Velcalcetide
Molecular Formula
C38H73N21O10S2 • XHCl
Formula Weight
1048.3
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
O=C([C@H](NC([C@H](NC([C@H](NC([C@@H](CSSC[C@@H](C(O)=O)N)NC(C)=O)=O)C)=O)CCCNC(N)=N)=O)CCCNC(N)=N)N[C@@H](C(N[C@@H](C(N[C@H](CCCNC(N)=N)C(N)=O)=O)C)=O)CCCNC(N)=N.Cl
InChi Code
InChI=1S/C38H73N21O10S2.ClH/c1-18(28(62)56-22(27(40)61)8-4-12-49-35(41)42)53-30(64)23(9-5-13-50-36(43)44)58-32(66)25(11-7-15-52-38(47)48)59-31(65)24(10-6-14-51-37(45)46)57-29(63)19(2)54-33(67)26(55-20(3)60)17-71-70-16-21(39)34(68)69;/h18-19,21-26H,4-17,39H2,1-3H3,(H2,40,61)(H,53,64)(H,54,67)(H,55,60)(H,56,62)(H,57,63)(H,58,66)(H,59,65)(H,68,69)(H4,41,42,49)(H4,43,44,50)(H4,45,46,51)(H4,47,48,52);1H/t18-,19-,21+,22-,23-,24-,25-,26-;/m1./s1
InChi Key
KHQMSZGKHGQUHG-WZDHWKSBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $351

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    Product Description

    Etelcalcetide is a peptide agonist of the calcium-sensing receptor (CaSR).1 It is selective for CaSR over a panel of 33 receptors and ion channels, as well as the norepinephrine transporter at 10 µM. Etelcalcetide increases intracellular calcium levels in HEK293T cells expressing the human CaSR receptor with an EC50 value of 0.53 µM. It also inhibits parathyroid secretion from primary rat parathyroid cells (EC50 = 0.36 µM in the presence of calcium). Etelcalcetide (0.3, 1, and 3 mg/kg) decreases parathyroid hormone and calcium levels in plasma and serum, respectively, in a model of chronic renal insufficiency with secondary hyperthyroidism in nephrectomized rats fed a high-phosphorus diet. Formulations containing etelcalcetide have been used in the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease undergoing hemodialysis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Harada, K., Fujioka, A., Konno, M., et al. Pharmacology of Parsabiv® (etelcalcetide, ONO-5163/AMG 416), a novel allosteric modulator of the calcium-sensing receptor, for secondary hyperparathyroidism in hemodialysis patients. Eur. J. Pharmacol. 842, 139-145 (2019).