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Description: Cinacalcet HCl (also known as AMG-073 HCl; trade names Sensipar, Mimpara) is a calcimimetic that mimics the action of calcium on tissues by allosteric activation of the calcium-sensing receptor expressed in various human organ tissues. It is a novel class of compounds for the treatment of hyperparathyroidism. Cinacalcet is a type II calcimimetic agent which controls calcium levels in cells by allosteric activation of CaSR. In the presence of calcium ions, it can inhibit parathyroid hormone secretion by activating CaSR in parathyroid glands. Cinacalcet has been used clinically to treat secondary hyperparathyroidism due to end-stage renal disease or hypercalcemia in patients with parathyroid carcinoma.
References: Kidney Int Suppl. 2003 Jun;(85):S91-6; Clin Ther. 2005 Nov;27(11):1725-51.
Related CAS#: 226256-56-0 (free base); 364782-34-3 (HCl)
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: AMG-073 represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium. AMG-073 has potential advantages as a therapy for secondary hyperparathyroidism because it mimics the effects of extracellular calcium to suppress PTH secretion, even in the presence of hyperphosphatemia, without the risk of causing hypercalcemia and/or hyperphosphatemia. AMG-073 produces a concentration-dependent increase in cytoplasmic calcium in human embryonic kidney cells expressing the CaSR. In bovine parathyroid cells and a buffer containing calcium 0.5 mM, AMG 073 (3 nM – 1 μM) produces a concentration-dependent decrease in PTH levels with IC50 of 27 nM.
Kidney Int Suppl. 2003 Jun;(85):S91-6; Clin Ther. 2005 Nov;27(11):1725-51.
Lot#: V149101, Purity ≥98%
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