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Cinacalcet (AMG-073) HCl CaSR activator

Cat.No.S1260

Cinacalcet (Mimpara, Sensipar,AMG-073) HCl represents a new class of compounds for the treatment of hyperparathyroidism.
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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (200.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 393.87 Formula

C22H22F3N.HCl

Storage (From the date of receipt)
CAS No. 364782-34-3 Download SDF Storage of Stock Solutions

Synonyms Mimpara, Sensipar,AMG-073 SMILES CC(C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl

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Mechanism of Action

Targets/IC50/Ki
CaSR
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.

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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-06-02)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06288451 ACTIVE_NOT_RECRUITING
Kidney Failure, Chronic; Chronic Kidney Disease-Mineral and Bone Disorder
University of Washington
2024-03-11 PHASE2
NCT07122401 RECRUITING
Secondary Hyperparathyroidism, Chronic Kidney Disease
Shaanxi Micot Pharmaceutical Technology Co., Ltd.
2025-09-30 PHASE3
NCT06434961 COMPLETED
Secondary Hyperparathyroidism
Shanghai Hengrui Pharmaceutical Co., Ltd.
2024-06-14 PHASE3
NCT03994172 COMPLETED
Male Osteoporosis
VA Office of Research and Development
2019-07-01 PHASE4
NCT05926570 COMPLETED
Drug Effect
Tanta University
2023-08-05 PHASE4
NCT05663411 UNKNOWN
Secondary Hyperparathyroidism
Shanghai Hengrui Pharmaceutical Co., Ltd.
2023-02-24 PHASE2

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