Cinacalcet HCl (AMG-073)

Alias: AMG073 HCl; Cinacalcet Hydrochloride; Sensipar; AMG-073 HCl; AMG 073 HCl; KRN1493; KRN-1493; Cinacalcet HCl; Mimpara; Regpara; cinacalcet; cinacalcet hydrochloride; Hydrochloride, Cinacalcet; KRN 1493

Cat No.:V1491 Purity: = 100%

COA Product Data Instructions for use SDS

Cinacalcet HCl (AMG-073) Chemical Structure CAS No.: 364782-34-3
Product category: CaSR

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Cinacalcet HCl (AMG-073):

Cinacalcet (AMG-073)

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

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Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: = 100%

COA

MSDS

NMR

HPLC

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information

Product Description

Cinacalcet HCl (also known as AMG-073; KRN1493; KRN-1493; Regpara; trade names Sensipar, Mimpara), the hydrochloride salt of Cinacalcet, is a calcimimetic that mimics the action of calcium on tissues by allosteric activation of the calcium-sensing receptor expressed in various human organ tissues. It is a medicine that has been approved to treat primary hyperparathyroidism, parathyroid carcinoma, and hyperparathyroidism. By allosterically activating CaSR, cinacalcet, a type II calcimimetic agent, regulates the amount of calcium present in cells. It can stop the release of parathyroid hormone by activating CaSR in the parathyroid glands when calcium ions are present. Clinical trials have employed cinacalcet to treat patients with parathyroid carcinoma who have hypercalcemia or secondary hyperparathyroidism brought on by end-stage renal disease.

Biological Activity I Assay Protocols (From Reference)

Targets

CaSR ( EC50 = 2.8 μM )

ln Vitro

In vitro activity: AMG-073 belongs to a novel class of drugs called calcimimetics that are used to treat hyperparathyroidism. These drugs decrease the production and secretion of parathyroid hormone (PTH) by making the parathyroid calcium-sensing receptor (CaR) more sensitive to extracellular calcium. Because AMG-073 mimics the effects of extracellular calcium to suppress PTH secretion even in the presence of hyperphosphatemia without running the risk of causing hyperphosphatemia or hypercalcemia, it has potential benefits as a therapy for secondary hyperparathyroidism. Human embryonic kidney cells expressing the CaSR exhibit a concentration-dependent rise in cytoplasmic calcium upon exposure to AMG-073. With an IC50 of 27 nM, AMG 073 (3 nM – 1 μM) causes a concentration-dependent drop in PTH levels in bovine parathyroid cells in a buffer containing 0.5 mM of calcium.[2]

ln Vivo

AMG-073 orally administered to normal rats at doses of 1, 3, 10, and 30 mg/kg in 20% sulfobutyl ether β-cyclodextrin sodium causes a notable dose-dependent decrease in PTH levels that lasts for one to four hours. The 10- and 30-mg/kg doses of AMG-073 cause notable drops in PTH levels at 8 hours when compared to controls; these reductions disappear after 24 hours. After oral administration of AMG-073, 10, 30, and 40 mg/kg, respectively, there is a significant dose-dependent reduction in serum calcium levels at 4, 8, and 24 hours later. Only at the maximum dose of AMG-073 is a temporary drop in serum phosphorus levels seen. Furthermore, rats given 40 mg/kg of AMG-073 showed elevated calcitonin levels that correlated with PTH suppression. After receiving AMG-073 orally, five out of six nephrectomized rats showed a swift, dose-dependent decrease in PTH and calcium levels, just like in normal rats. Furthermore, compared to controls, oral AMG-073 at 5 and 10 mg/kg for 4 weeks results in a significant reduction in parathyroid weight. [2]

Animal Protocol

Nuclear DNA fragmentation is measured in situ using the Apoptag System 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). In short, parathyroid gland sections from animals treated with vehicle or cinacalcet HCl are digested for 15 minutes at room temperature using 20 μg/mL proteinase K in 0.1 mol/L PBS. To block endogenous peroxidase, the sections are then incubated with 3% hydrogen peroxide/methanol for 5 minutes. To tag exposed 3′-OH DNA ends with digoxigenin-tagged nucleotides, sections are incubated with terminal deoxynucleotidyl transferase (TdT) for 1 hour at 37°C. The immunoperoxidase method finds DNA that has been labeled with digoxigenin. The nuclei of apoptotic cells are stained brown, and sections are created using 3,3′-diaminobenzidine (DAB). When TdT is replaced with distilled water, the specificity for apoptosis is confirmed using negative staining.

References

[1]. Kidney Int Suppl . 2003 Jun:(85):S91-6.

[2]. Clin Ther . 2005 Nov;27(11):1725-51.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C22H23CLF3N
Molecular Weight	393.87
Exact Mass	393.15
Elemental Analysis	C, 67.09; H, 5.89; Cl, 9.00; F, 14.47; N, 3.56
CAS #	364782-34-3
Related CAS #	Cinacalcet; 226256-56-0; Cinacalcet-d3 hydrochloride; Cinacalcet-d3
Appearance	Solid powder
SMILES	C[C@H](C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl
InChi Key	QANQWUQOEJZMLL-PKLMIRHRSA-N
InChi Code	InChI=1S/C22H22F3N.ClH/c1-16(20-13-5-10-18-9-2-3-12-21(18)20)26-14-6-8-17-7-4-11-19(15-17)22(23,24)25;/h2-5,7,9-13,15-16,26H,6,8,14H2,1H3;1H/t16-;/m1./s1
Chemical Name	N-[(1R)-1-naphthalen-1-ylethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine;hydrochloride
Synonyms	AMG073 HCl; Cinacalcet Hydrochloride; Sensipar; AMG-073 HCl; AMG 073 HCl; KRN1493; KRN-1493; Cinacalcet HCl; Mimpara; Regpara; cinacalcet; cinacalcet hydrochloride; Hydrochloride, Cinacalcet; KRN 1493
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~79 mg/mL (~200.6 mM)

Water: <1 mg/mL

Ethanol: ~33 mg/mL (~83.8 mM)

Solubility (In Vivo)

30% PEG400+0.5% Tween80+5%Propylene glycol: 30mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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
	10 mM	0.2539 mL	1.2695 mL	2.5389 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05663411	Active Recruiting	Drug: SHR6508 Drug: Cinacalcet	Secondary Hyperparathyroidism	Shanghai Hengrui Pharmaceutical Co., Ltd.	February 24, 2023	Phase 2
NCT05926570	Recruiting	Drug: Cinacalcet	Drug Effect	Tanta University	August 5, 2023	Phase 4
NCT03994172	Recruiting	Drug: Cinacalcet Drug: placebo tablet	Male Osteoporosis	VA Office of Research and Development	July 1, 2019	Phase 4
NCT00977080	Completed	Drug: Paricalcitol Drug: Cinacalcet	Chronic Kidney Disease Hemodialysis	Abbott	November 2009	Phase 4
NCT03299244	Completed	Drug: Cinacalcet Drug: Etelcalcetide	Secondary Hyperparathyroidism Chronic Kidney Disease	Amgen	May 15, 2018	Phase 3