Cinacalcet HCl (Synonyms: AMG 073, KRN 1493, Mimpara) |
Catalog No.GC16708
One-Click Copy Product Info
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Cinacalcet HCl (clorhidrato de AMG-073) es un agonista alostérico del receptor de Ca (CaR), activo por vÍa oral, que se utiliza para el tratamiento de enfermedades cardiovasculares.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 364782-34-3
Sample solution is provided at 25 µL, 10mM.
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Cinacalcet HCl (AMG 073), the second-generation calcimimetic, is a potent agonist of calcium-sensing receptor (CaR) with an EC50 value of 2.8 μm [1].
Cinacalcet HCl showed to be safe for the secondary hyperparathyroidism treatment. Besides, cinacalcet HCl has been proved to reduce parathyroid hormone (PTH) levels significantly while reducing the calcium x phosphorus product and serum phosphorus levels at the same time [1].
Administered orally with cinacalcet in Rice H-500 tumor bearing mice has shown a significant reduction of blood ionized calcium, serum total calcium concentrations and serum PTHrP levels [2].
References:
[1] Ureña P1, Frazão JM. Calcimimetic agents: review and perspectives. Kidney Int Suppl. 2003 Jun;(85):S91-6.
[2] Colloton M1, Shatzen E, Wiemann B, Starnes C, Scully S, Henley C, Martin D.Cinacalcet attenuates hypercalcemia observed in mice bearing either Rice H-500 Leydig cell or C26-DCT colon tumors. Eur J Pharmacol. 2013 Jul 15;712(1-3):8-15.
Animal experiment: | 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. |
References: [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. | |
| Cas No. | 364782-34-3 | SDF | |
| Sinónimos | AMG 073, KRN 1493, Mimpara | ||
| Chemical Name | N-[(1R)-1-naphthalen-1-ylethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine;hydrochloride | ||
| Canonical SMILES | CC(C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl | ||
| Formula | C22H23ClF3N | M.Wt | 393.87 |
| Solubility | ≥ 17.85mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5389 mL | 12.6945 mL | 25.3891 mL |
| 5 mM | 507.8 μL | 2.5389 mL | 5.0778 mL |
| 10 mM | 253.9 μL | 1.2695 mL | 2.5389 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)