Cinacalcet-d3 is intended for use as an internal standard for the quantification of cinacalcet by GC- or LC-MS. Cinacalcet is a calcimimetic and an allosteric agonist of the calcium-sensing receptor (CaSR; EC50 = 79.4 nM in HEK293T cells expressing the human receptor).1 In vivo, cinacalcet (0.1-10 mg/kg, s.c.) decreases plasma levels of parathyroid hormone (PTH) in rats. It also decreases plasma levels of PTH and parathyroid cell proliferation in a mouse model of primary hyperparathyroidism.2 Formulations containing cinacalcet have been used in the treatment of secondary hyperparathyroidism due to end-stage renal disease and hypercalcemia in patients with parathyroid carcinoma.
1.Ma, J.N., Owens, M., Gustafsson, M., et al.Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptorJ. Pharmacol. Exp. Ther.337(1)275-284(2011) 2.Imanishi, Y., Kawata, T., Kenko, T., et al.Cinacalcet HCl suppresses Cyclin D1 oncogene-derived parathyroid cell proliferation in a murine model for primary hyperparathyroidismCalcif. Tissue Int.89(1)29-35(2011)