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Cinacalcet

Name: Cinacalcet
Brand: TargetMol
SKU: T8403
Price: 43 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8403Cas No. 226256-56-0

Alias AMG 073

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

Cinacalcet

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Purity: 99.48%

Catalog No. T8403Alias AMG 073Cas No. 226256-56-0

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

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$43	In Stock	In Stock
25 mg	$64	In Stock	In Stock
50 mg	$80	In Stock	In Stock
100 mg	$147	In Stock	In Stock
500 mg	$369	-	In Stock
1 mL x 10 mM (in DMSO)	$47	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.48%

Appearance:Liquid

Color:Transparent

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COA HNMR HPLC LCMS

Product Introduction

Cinacalcet AI Summary

Cinacalcet exhibits a diverse range of bioactivities, including inhibitory effects on ROR gamma transcriptional activity, Histone Lysine Methyltransferase G9a, TGF-b, USP1/UAF1, human tyrosyl-DNA phosphodiesterase 1 (TDP1), and the malarial parasite plastid. It induces DNA re-replication in various cell types and modulates PINK1 expression, indicating broad biological effects. Notably, Cinacalcet acts as a positive allosteric modulator of the human Calcium-sensing receptor (CaSR) in CHO cells with an EC50 value of 80.0 nM, and potentiates human GlyR-alpha1 expressed in Xenopus laevis oocytes, showing an activity of 182.0% at 1 µM and a maximum activity of 210.0% at 10 µM. The compound also inhibits recombinant human P450 CYP2D6 enzyme with an IC50 value of 50.0 nM. In terms of toxicity, Cinacalcet shows a lack of bioactivity in hepatic side effect assays, suggesting a low risk for drug-induced liver injury and related conditions. Furthermore, it demonstrates minimal efficacy against SARS-CoV-2, with weak inhibition of virus-induced cytotoxicity in VERO-6 cells and moderate inhibition of the SARS-CoV-2 3CL-Pro protease. Cinacalcet also displays inhibitory activity against enzymes such as human HDAC6 and porcine heart malate dehydrogenase, with IC50 values of >20000 nM and 74,000 nM, respectively. Additionally, it shows antagonist activity at human HRH1 and CHRM2 receptors and agonist activity at human OPRM1 and CHRM2 receptors. The compound has been evaluated for binding affinity and inhibition of numerous targets, including KCNH2, ADRB1, SLC6A3, HTR2C, SLC6A4, ADRA2C, PTGS2, HTR3A, and MAOA, highlighting its extensive interaction profile. Overall, Cinacalcet displays a wide array of biological activities across different assays, making it a compound of interest for further exploration in various therapeutic areas..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Cinacalcet (AMG 073) is an orally active, allosteric Ca receptor (CaR) agonist used in the treatment of cardiovascular disease.
Synonyms	AMG 073

Chemical Properties

Molecular Weight	357.41
Formula	C₂₂H₂₂F₃N
Cas No.	226256-56-0
Smiles	[C@@H](NCCCC1=CC(C(F)(F)F)=CC=C1)(C)C=2C3=C(C=CC2)C=CC=C3
Relative Density.	1.154 g/cm3

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (279.79 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (11.19 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7979 mL	13.9895 mL	27.9791 mL	139.8954 mL
5 mM	0.5596 mL	2.7979 mL	5.5958 mL	27.9791 mL
10 mM	0.2798 mL	1.3990 mL	2.7979 mL	13.9895 mL
20 mM	0.1399 mL	0.6995 mL	1.3990 mL	6.9948 mL
50 mM	0.0560 mL	0.2798 mL	0.5596 mL	2.7979 mL
100 mM	0.0280 mL	0.1399 mL	0.2798 mL	1.3990 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc