Cinacalcet HCl

Catalog No.S1260 Synonyms: AMG-073 HCl

Cinacalcet HCl Chemical Structure

Molecular Weight(MW): 393.87

Cinacalcet HCl represents a new class of compounds for the treatment of hyperparathyroidism.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 670 In stock
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1 Customer Review

  • A. SK-N-LP cells stably transfected with pCMV-GFP or pCMV-CaSR-GFP were grown in serum deprivation media for 16 hours. They were then exposed to cinacalcet for 24 hours at indicated doses in the same media containing 0.5 mM CaCl2 . Total proteins were isolated from floating and adherent cells to conduct immunoblots.

    Oncotarget, 2016, 7(13):16112-29. Cinacalcet HCl purchased from Selleck.

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Biological Activity

Description Cinacalcet HCl represents a new class of compounds for the treatment of hyperparathyroidism.
Targets
CaSR [1]
()
2.8 μM(EC50)
In vitro

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. [2]

In vivo AMG-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. [2]

Protocol

Solubility (25°C)

In vitro DMSO 79 mg/mL (200.57 mM)
Ethanol 33 mg/mL (83.78 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 393.87
Formula

C22H22F3N.HCl

CAS No. 364782-34-3
Storage powder
in solvent
Synonyms AMG-073 HCl

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02525796 Recruiting Primary Hyperparathyroidism Brigham and Womens Hospital January 2016 Phase 2|Phase 3
NCT02440581 Recruiting Kidney Failure, Chronic Hartmut Malluche, MD|Wright State University|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|University of Kentucky July 2015 --
NCT02341417 Active, not recruiting Secondary Hyperparathyroidism, Chronic Kidney Disease Amgen June 2015 Phase 3
NCT02338934 Unknown status Secondary Hyperparathyroidism Penang Hospital, Malaysia|Ministry of Health, Malaysia January 2015 Phase 4
NCT02138838 Terminated Chronic Kidney Disease, Secondary Hyperparathyroidism Amgen November 2014 Phase 3
NCT02227264 Recruiting Primary Hyperparathyroidism Karolinska University Hospital|Karolinska Institutet June 2014 --

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CaSR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID