1. GPCR/G Protein Metabolic Enzyme/Protease
  2. CaSR Endogenous Metabolite
  3. Cinacalcet hydrochloride

Cinacalcet hydrochloride  (Synonyms: AMG-073 hydrochloride)

Cat. No.: HY-70037A Purity: 99.99%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Cinacalcet hydrochloride Chemical Structure

Cinacalcet hydrochloride Chemical Structure

CAS No. : 364782-34-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 61 In-stock
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10 mg USD 55 In-stock
50 mg USD 100 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of Cinacalcet hydrochloride:

Top Publications Citing Use of Products

    Cinacalcet hydrochloride purchased from MedChemExpress. Usage Cited in: Calcif Tissue Int. 2023 Feb 8.  [Abstract]

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

    Cinacalcet hydrochloride 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    In Vivo

    Cinacalcet (5 and 10 mg/kg) results in a significant reduction in parathyroid gland weight in 5/6 nephrectomy animals. In sham animals, Cinacalcet 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 (10, 5, or 1 mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6 nephrectomized animals. Cinacalcet 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.

    Clinical Trial
    Molecular Weight

    393.87

    Formula

    C22H23ClF3N

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (126.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 1 mg/mL (2.54 mM; ultrasonic and warming and heat to 60°C)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5389 mL 12.6945 mL 25.3891 mL
    5 mM 0.5078 mL 2.5389 mL 5.0778 mL
    View the Complete Stock Solution Preparation Table

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

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

    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: ≥ 2.5 mg/mL (6.35 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.35 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.99%

    References
    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 (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.

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

    References

    Complete Stock Solution Preparation Table

    * 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.5389 mL 12.6945 mL 25.3891 mL 63.4727 mL
    DMSO 5 mM 0.5078 mL 2.5389 mL 5.0778 mL 12.6945 mL
    10 mM 0.2539 mL 1.2695 mL 2.5389 mL 6.3473 mL
    15 mM 0.1693 mL 0.8463 mL 1.6926 mL 4.2315 mL
    20 mM 0.1269 mL 0.6347 mL 1.2695 mL 3.1736 mL
    25 mM 0.1016 mL 0.5078 mL 1.0156 mL 2.5389 mL
    30 mM 0.0846 mL 0.4232 mL 0.8463 mL 2.1158 mL
    40 mM 0.0635 mL 0.3174 mL 0.6347 mL 1.5868 mL
    50 mM 0.0508 mL 0.2539 mL 0.5078 mL 1.2695 mL
    60 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0579 mL
    80 mM 0.0317 mL 0.1587 mL 0.3174 mL 0.7934 mL
    100 mM 0.0254 mL 0.1269 mL 0.2539 mL 0.6347 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Cinacalcet hydrochloride Related Classifications

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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