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Cinacalcet HCl Sale

(Synonyms: 盐酸西那卡塞; AMG-073 hydrochloride) 目录号 : GC16708

An allosteric agonist of the CaSR

Cinacalcet HCl Chemical Structure

Cas No.:364782-34-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥609.00
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50mg
¥788.00
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500mg
¥3,759.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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.
[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.

产品描述

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.

Chemical Properties

Cas No. 364782-34-3 SDF
别名 盐酸西那卡塞; AMG-073 hydrochloride
化学名 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
分子式 C22H23ClF3N 分子量 393.87
溶解度 ≥ 17.85mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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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
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