生物活性 | |||
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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 | |||
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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 |
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