Catalog No.S1260 Synonyms: AMG-073 HCl
Molecular Weight(MW): 393.87
Cinacalcet HCl represents a new class of compounds for the treatment of hyperparathyroidism.
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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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|Description||Cinacalcet HCl represents a new class of compounds for the treatment of hyperparathyroidism.|
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 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. |
|In vitro||DMSO||79 mg/mL (200.57 mM)|
|Ethanol||33 mg/mL (83.78 mM)|
|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.
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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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