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Cinacalcet (AMG-073) HCl

Name: Cinacalcet (AMG-073) HCl
Brand: Selleck Chemicals
SKU: S1260
Rating: 5 (6 reviews)

Synonyms: Mimpara, Sensipar,AMG-073

Catalog No.S1260 Purity: 99.99%

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

Cinacalcet (AMG-073) HCl Chemical Structure

CAS: 364782-34-3

Selleck's Cinacalcet (AMG-073) HCl has been cited by 6 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Biological Activity

Description

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

Targets

CaSR ^[1]

2.8 μM(EC50)

In vitro
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05926570	Recruiting	Drug Effect	Tanta University	August 5 2023	Phase 4
NCT03123406	Completed	Hyperparathyroidism; Secondary Renal	Kyowa Kirin China Pharmaceutical Co. Ltd.	April 19 2017	Phase 4
NCT02341417	Completed	Secondary Hyperparathyroidism Chronic Kidney Disease	Amgen	June 10 2015	Phase 3
NCT01748812	Terminated	Osteomalacia	National Institute of Dental and Craniofacial Research (NIDCR)\|National Institutes of Health Clinical Center (CC)	November 16 2012	Phase 1
NCT01439867	Terminated	Chronic Kidney Disease\|Hyperparathyroidism Secondary	Amgen	June 22 2012	Phase 2

References

Chemical lnformation & Solubility

Molecular Weight	393.87	Formula	C₂₂H₂₂F₃N.HCl
CAS No.	364782-34-3	SDF	Download Cinacalcet (AMG-073) HCl SDF
Smiles	CC(C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 79 mg/mL ( (200.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble

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In vivo
Batch:

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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.

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