Cinacalcet (AMG-073) HCl
For research use only.
CAS No. 364782-34-3
Cinacalcet (AMG-073) HCl represents a new class of compounds for the treatment of hyperparathyroidism.
Selleck's Cinacalcet (AMG-073) HCl has been cited by 5 publications
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Effects of intra-synovial injections of CaSR antagonist (NPS2143) and agonist (Cinacalcet) on morphology (A) in rat TMJ cartilage without (Control) or with UAC stimulation. Test compounds (50 μL of 100 nM stock) and vehicle injections were performed on 10‐week‐old rats every other day for 4 weeks. UAC began 4 weeks before drug injections and continued for another 4 weeks during drug treatments. (A) Safranin O staining (in red) showed the ability of NPS2143 to increase proteoglycan content and thickness of TMJ cartilage and decreased OA grade, the ability of Cinacalcet to suppress these parameters in both control and UAC groups when compared with corresponding vehicle‐injected group. Scale bar = 100 µm. n = 6 rats per group.
J Bone Miner Res, 2018, doi:10.1002/jbmr.3643. Cinacalcet (AMG-073) HCl purchased from Selleck.
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 (AMG-073) HCl purchased from Selleck.
Cells were exposed to vehicle or cinacalcet 2 μM for 2 and 16 h (A and B) either alone (white bars) or adding CQ 20 μM (gray bars) for the last 3 h. Each panel shows a representative image of LC3II and β-actin (internal loading control) and the respective densitometry analysis. Bars represent mean ± SEM of 5–7 independent experiments. *p < 0.05 vs. all other conditions. Two-way ANOVA and Tukey's post hoc test for multiple comparisons.
Biochim Biophys Acta Mol Basis Dis, 2018, 1864(11):3585-3594. Cinacalcet (AMG-073) HCl purchased from Selleck.
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Choose Selective CaSR Inhibitors
|Description||Cinacalcet (AMG-073) 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)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03123406||Completed||Drug: Cinacalcet HCl||Hyperparathyroidism; Secondary Renal||Kyowa Hakko Kirin China Pharmaceutical Co. LTD.||April 19 2017||Phase 4|
|NCT02341417||Completed||Drug: Cinacalcet||Secondary Hyperparathyroidism Chronic Kidney Disease||Amgen||June 10 2015||Phase 3|
|NCT01748812||Terminated||Drug: Osteomalacia||Osteomalacia||National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC)||November 16 2012||Phase 1|
|NCT01599962||Completed||Drug: Cinacalcet|Drug: Placebo||Memory Functions||Prof. Dominique de Quervain MD|Clinical Trial Unit University Hospital Basel Switzerland|University of Basel||March 2012||Phase 2|
|NCT01519037||Completed||Drug: Cinacalcet 60 MG|Drug: Placebo oral tablet||Relationship Between Calcimimetic and the RAAS||Centre Hospitalier Universitaire Vaudois|Swiss National Science Foundation||January 2012||Not Applicable|
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