Art. -Nr.: HY-70037

Cinacalcet

(Synonyms: AMG 073)

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.

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Reinheit: 99.93%
CAS. Nr.: 226256-56-0
Formel: C₂₂H₂₂F₃N
Molecular Weight:357.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cinacalcet Chemical Structure

CAS. Nr.: 226256-56-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vivo
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research.

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	80 nM Compound: AMG-073, Sensipar	Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay	[PMID: 23465611]
Vero	CC₅₀	4.25 μM Compound: Cinacalcet	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 37659195]

In Vivo

Cinacalcet HCl (5 and 10 mg/kg) results in a significant reduction in parathyroid gland weight in 5/6 nephrectomy animals. In sham animals, Cinacalcet HCl has no effect on parathyroid gland cell proliferation or parathyroid weight compared with vehicle treatment. There are no differences in serum phosphorus levels in Cinacalcet HCl (10, 5, or 1 mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6 nephrectomized animals. Cinacalcet HCl treatment significantly reduces blood ionized calcium levels in sham animals^[1]. Cinacalcet (30 mg/kg/24 h) leads to a marked reduction in circulating parathyroid hormone and a modest reduction in serum Ca. Cinacalcet does not alter UCa when the GHS rats are fed the normal Ca diet but lowers UCa when they are fed the low Ca diet. Cinacalcet does not alter U supersaturation with respect to either CaOx or CaHPO4 on either diet^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 226256-56-0
Appearance Solid
Molecular Weight 357.41
Formel C₂₂H₂₂F₃N
Color White to off-white
SMILES

FC(F)(C1=CC(CCCN[C@@H](C2=C3C=CC=CC3=CC=C2)C)=CC=C1)F
Synonyms

AMG 073
Structure Classification
- Others
Initial Source
- Endogenous metabolite
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

All WB

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Journal Impact Factor

Adv Mater

Efficient Delivery of Lomitapide using Hybrid Membrane-Coated Tetrahedral DNA Nanostructures for Glioblastoma Therapy. [Abstract]

2024 Jun;36(24):e2311760. PMID: 38569065
J Med Chem

Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. [Abstract]

2015 Apr 9;58(7):2958-66. PMID: 25790278
J Agric Food Chem

Tryptophan Promotes Intestinal Immune Defense through Calcium-Sensing Receptor (CaSR)-Dependent Metabolic Pathways. [Abstract]

2021 Nov 17;69(45):13460-13473. PMID: 34748328
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Acta Physiol

The CaSR/TRPV4 coupling mediates pro-inflammatory macrophage function. [Abstract]

2023 Apr;237(4):e13926. PMID: 36606511
Cell Biol Toxicol

Neurorescuing effect of Cinacalcet against hypercalcemia-induced nerve injury in chronic kidney disease via TRAF2/cIAP1/KLF2/SERPINA3 signal axis. [Abstract]

2023 Oct;39(5):1-17. PMID: 35635602
J Clin Endocrinol Metab

Heterogenous Origins of Calcium Homeostasis Disorders Arising from Five Heterozygous Calcium-Sensing Receptor Variants. [Abstract]

2024 Oct 16:dgae735. PMID: 39413244
iScience

Cinacalcet exhibits rapid bactericidal and efficient anti-biofilm activities against multidrug-resistant Gram-positive pathogens. [Abstract]

2023 Mar 11;26(4):106378. PMID: 37034999
J Food Sci

Sensing of L-Arginine by Gut-Expressed Calcium Sensing Receptor Stimulates Gut Satiety Hormones Cholecystokinin and Glucose-Dependent Insulinotropic Peptide Secretion in Pig Model. [Abstract]

2018 Sep;83(9):2394-2401. PMID: 30088839
J Biol Chem

Positive Allosteric Modulation of the Calcium-sensing Receptor by Physiological Concentrations of Glucose. [Abstract]

2016 Oct 28;291(44):23126-23135. PMID: 27613866
J Funct Foods

2025 Apr.
Calcif Tissue Int

Rescue of High Glucose Impairment of Cultured Human Osteoblasts Using Cinacalcet and Parathyroid Hormone. [Abstract]

2023 Apr;112(4):452-462. PMID: 36754901

Cinacalcet purchased from MedChemExpress. Usage Cited in: Calcif Tissue Int. 2023 Apr;112(4):452-462. [Abstract]

Cinacalcet (CN) and parathyroid hormone (PTH), used together or separately at physiological glucose levels, produce an increase expression of RUNX2 in HOBs.
Gen Comp Endocrinol

Phenylalanine and tryptophan stimulate gastrin and somatostatin secretion and H+-K+-ATPase activity in pigs through calcium-sensing receptor. [Abstract]

2018 Oct 1:267:1-8. PMID: 29782837
bioRxiv

2025 Sep 21.
Patent

US20230147129A1.
Oxid Med Cell Longev

Exosomes Released from CaSR-Stimulated PMNs Reduce Ischaemia/Reperfusion Injury. [Abstract]

2021 Jan 12;2021:3010548. PMID: 33505580
Oxid Med Cell Longev

Expression and Role of the Calcium-Sensing Receptor in Rat Peripheral Blood Polymorphonuclear Neutrophils. [Abstract]

2017:2017:3869561. PMID: 29081886

Cinacalcet purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017:2017:3869561. [Abstract]

N-formyl-Met-Leu-Phe (fMLP; 10 nM) are used to stimulate the cells for 2 min, and the polymorphonuclear neutrophils (PMNs) without fMLP serve as the control. NPS-2143 (100 nM), Cinacalcet (100 nM), and PDTC (100 nM) are added and incubated. Protein expression results are representative of three experiments.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (279.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7979 mL

13.9895 mL

27.9791 mL

5 mM

0.5596 mL

2.7979 mL

5.5958 mL

10 mM

0.2798 mL

1.3990 mL

2.7979 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (7.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (7.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (7.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[1]

To identify apoptosis in parathyroid glands from 5/6 nephrectomized or sham rats treated with vehicle [phosphate-buffered saline (PBS)] or cinacalcet HCl (10 mg/kg), nuclear DNA fragmentation is measured in situ using the Apoptag System. Briefly, parathyroid gland sections from animals treated with vehicle or cinacalcet HCl are digested with 20 μg/mL proteinase K in 0.1 mol/L PBS at room temperature for 15 minutes and incubated with 3% hydrogen peroxide/methanol for 5 minutes to block endogenous peroxidase. Sections are incubated for 1 hour at 37°C with terminal deoxynucleotidyl transferase (TdT) to label exposed 3′-OH DNA ends with digoxigenin-tagged nucleotides. Digoxigenin-labeled DNA is detected by the immunoperoxidase method. Sections are developed with 3,3′-diaminobenzidine (DAB), and the nuclei of apoptotic cells are stained brown. The specificity for apoptosis is verified by negative staining when distilled water is substituted for TdT.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Colloton M, et al. Cinacalcet HCl attenuates parathyroid hyperplasia in a rat model of secondary hyperparathyroidism. Kidney Int. 2005 Feb;67(2):467-76. [Content Brief]

[2]. D.A. Bushinsky, et al. Effect of cinacalcet on urine calcium excretion and supersaturation in genetic hypercalciuric stone-forming rats. Kidney Int. 2006 May;69(9):1586-92. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7979 mL	13.9895 mL	27.9791 mL	69.9477 mL
	5 mM	0.5596 mL	2.7979 mL	5.5958 mL	13.9895 mL
	10 mM	0.2798 mL	1.3990 mL	2.7979 mL	6.9948 mL
	15 mM	0.1865 mL	0.9326 mL	1.8653 mL	4.6632 mL
	20 mM	0.1399 mL	0.6995 mL	1.3990 mL	3.4974 mL
	25 mM	0.1119 mL	0.5596 mL	1.1192 mL	2.7979 mL
	30 mM	0.0933 mL	0.4663 mL	0.9326 mL	2.3316 mL
	40 mM	0.0699 mL	0.3497 mL	0.6995 mL	1.7487 mL
	50 mM	0.0560 mL	0.2798 mL	0.5596 mL	1.3990 mL
	60 mM	0.0466 mL	0.2332 mL	0.4663 mL	1.1658 mL
	80 mM	0.0350 mL	0.1749 mL	0.3497 mL	0.8743 mL
	100 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6995 mL

Keywords

Cinacalcet

17 Cited Publications

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Cinacalcet

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Natural Product Diversity Scaffold Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Cinacalcet

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cinacalcet

GPCR/G Protein Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

Natural Product Diversity Scaffold Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Cinacalcet

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cinacalcet Related Classifications

HY-70037 Related Classifications