Cinacalcet HCl
(Synonyms: 盐酸西那卡塞; AMG-073 hydrochloride) 目录号 : GC16708
An allosteric agonist of the CaSR
Cas No.:364782-34-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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 | |
| 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 |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet