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      Cinacalcet HCl (AMG-073)
      Cinacalcet HCl (AMG-073)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V1491
      CAS #: 364782-34-3Purity ≥98%

      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)

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      Molecular Weight (MW)393.87
      FormulaC22H22F3N.HCl
      CAS No.364782-34-3 (HCl salt)
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 79 mg/mL (200.6 mM)
      Water: <1 mg/mL
      Ethanol: 33 mg/mL (83.8 mM)
      Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL
      SynonymsAMG-073 HCl;  AMG 073 HCl;  AMG073 HCl; Cinacalcet Hydrochloride; Sensipar; Cinacalcet HCl; Mimpara; Regpara; cinacalcet; cinacalcet hydrochloride; Hydrochloride, Cinacalcet; KRN1493; KRN-1493; KRN 1493;
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      In Vitro

      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.

      In VivoAMG-073 orally administrated to normal rats at dose of 1, 3, 10, and 30 mg/kg in 20% sulfobutyl ether β-cyclodextrin sodium produces a significant dose-dependent reduction in PTH levels for 1 to 4 hours after administration. At 8 hours, the 10- and 30-mg/kg doses of AMG-073 produces significant reductions in PTH levels compared with controls that disappears by 24 hours. Significant dose-dependent reduction in serum calcium levels are observed at 4, 8, and 24 hours after oral administration of AMG-073 3, 10, and 30 mg/kg, respectively. A transient reduction in serum phosphorus levels is observed only with the highest dose of AMG-073. In addition, increased calcitonin levels that paralleled PTH suppression are observed with AMG-073 40 mg/kg in rats. As in normal rats, a rapid dose-dependent reduction in PTH and calcium levels is observed in 5 of 6 nephrectomized rats after oral administration of AMG-073. In addition, oral AMG-073 at 5 and 10 mg/kg for 4 weeks significantly reduces parathyroid weight compared with controls.
      Animal modelRats
      Formulation & DosageDissolved in 20% sulfobutyl ether β-cyclodextrin sodium; 1, 3, 10, and 30 mg/kg; oral
      References

      Kidney Int Suppl. 2003 Jun;(85):S91-6; Clin Ther. 2005 Nov;27(11):1725-51.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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