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Etelcalcetide

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Chemical Structure| 1262780-97-1 同义名 : AMG 416;KAI-4169
CAS号 : 1262780-97-1
货号 : A592953
分子式 : C38H73N21O10S2
纯度 : 98+%
分子量 : 1048.25
MDL号 : MFCD31735128
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Etelcalcetide is a positive allosteric modulator/peptide agonist of the CaR with EC50 value of 25μM for increasing IP1 accumulation in HEK-293 cells expressing the human CaR. It is approved for the treatment of secondary hyperpara-thyroidism in adults with chronic kidney disease on hemodialysis. The efficacy in vivo of Etelcalcetide is usually measured by the magnitude and duration of decreases in plasma plasma parathyroid hormone (PTH) levels. For example, a single dose of etelcalcetide at 0.5mg/kg caused a substantial drop in PTH levels in rats with acute renal dysfunction (1K1C model), and this effect by etelcalcetide remained approximately 50% below their initial level at 24 hrs.
作用机制 Etelcalcetide forms a covalent disulphide bond with the CaR.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.95mL

0.19mL

0.10mL

4.77mL

0.95mL

0.48mL

9.54mL

1.91mL

0.95mL

参考文献

[1]Block GA, Bushinsky DA, et al. Effect of Etelcalcetide vs Cinacalcet on Serum Parathyroid Hormone in Patients Receiving Hemodialysis With Secondary Hyperparathyroidism: A Randomized Clinical Trial. JAMA. 2017 Jan 10;317(2):156-164.

[2]Subramanian R, Zhu X, et al. Nonclinical Pharmacokinetics, Disposition, and Drug-Drug Interaction Potential of a Novel d-Amino Acid Peptide Agonist of the Calcium-Sensing Receptor AMG 416 (Etelcalcetide). Drug Metab Dispos. 2016 Aug;44(8):1319-31.