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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / CaSR / Cinacalcet hydrochloride

盐酸西那卡塞 /Cinacalcet hydrochloride {[allProObj[0].p_purity_real_show]}

货号：A164114 同义名： AMG-073 hydrochloride;Cinacalcet (hydrochloride)

Cinacalcet hydrochloride (AMG-073 hydrochloride)是一种口服活性、别构激动剂Ca受体（CaR），用于治疗心血管疾病。

Cinacalcet hydrochloride 化学结构 CAS号：364782-34-3
Cinacalcet hydrochloride 化学结构
CAS号：364782-34-3
Cinacalcet hydrochloride 3D分子结构
CAS号：364782-34-3
Cinacalcet hydrochloride 化学结构 CAS号：364782-34-3
Cinacalcet hydrochloride 3D分子结构 CAS号：364782-34-3
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Cinacalcet hydrochloride 纯度/质量文件 产品仅供科研

货号：A164114 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 CaSR ↓ 其他靶点 纯度
NPS-2143 ++++

Ca(2+) receptor, IC50: 43 nM

 		98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cinacalcet hydrochloride 生物活性

描述 Calcium-sensing receptor (CaSR), which belongs to the G protein-coupled receptor superfamily, is responsible for the regulation of systemic Ca2+ metabolism. Cinacalcet hydrochloride is a calcimimetic that allosterically increases the sensitivity and responsiveness of CaSR to Ca2+. It activates the wild-type CaSR signaling in cellular proliferation and PI hydrolysis assays with pEC50 values of 7.6 and 7.3, respectively[1]. When primary cultured human parathyroid cells were incubated with 0.5 mM extracellular Ca2+, cinacalcet hydrochloride from 0 – 1000 nM additionally suppressed the secretion of parathyroid hormone at a dose-dependent manner[2]. Cinacalcet hydrochloride at 30 – 1000 nM had no effect on osteoclastic formation or resorption in osteoclastic cells cultured in calcium-containing medium with the concentration of 1.6 or 6.1 mM[3]. Oral administration of primary hyperparathyroidism mice with 1 mg/g cinacalcet hydrochloride for 10 days led to significantly reduced levels of parathyroid and Ca in serum. The uptake of 5-Bromo-2’-deoxyuridine was also significantly decreased in mice following the administration of cinacalcet hydrochloride compared to the untreated ones[4].
作用机制 Cinacalcet hydrochloride cooperates with Ca2+ to activate CaSR via interacting with its transmembrane domain[1].

Cinacalcet hydrochloride 动物研究

Dose Rat: 1 mg/kg - 10 mg/kg[5] (p.o.); 0.1 mg/kg - 10 mg/kg[1] (s.c.) Mice: 10 mg/kg - 100 mg/kg (p.o.)
Administration p.o., s.c.
Pharmacokinetics
Animal Rats[6] Monkeys[6]
Dose 1 mg/kg 10 mg/kg
Administration i.v. or p.o. p.o.
T1/2 5.5 h (i.v.)
3.1 h (p.o.) 		9.1 h
Tmax 1.9 h (p.o.) 2.8 h
CL 1.00 L/h/kg (i.v.)
AUC 1570 ng·h/ml (i.v.)
21.5 ng·h/ml (p.o.) 		237.1 ng·h/ml

Cinacalcet hydrochloride 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01100723 - Completed - -
NCT02464072 Hyperparathyroidism, Secondary Not Applicable Active, not recruiting July 2019 Brazil ... 展开 >> University of Sao Paulo General Hospital Sao Paulo, SP, Brazil 收起 <<
NCT01073462 - Completed - Austria ... 展开 >> Site Reference ID/Investigator# 27447 Graz, Austria, 8010 Site Reference ID/Investigator# 49182 Graz, Austria, 8020 Site Reference ID/Investigator# 27483 Graz, Austria, 80360 Site Reference ID/Investigator# 52742 Graz, Austria, 8052 Site Reference ID/Investigator# 27487 Innsbruck, Austria, 6020 Site Reference ID/Investigator# 36983 Linz, Austria, 4010 Site Reference ID/Investigator# 27484 Linz, Austria, 4020 Site Reference ID/Investigator# 27485 Rottenmann, Austria, 8786 Site Reference ID/Investigator# 27446 Vienna, Austria, 1030 Site Reference ID/Investigator# 53469 Vienna, Austria, 1090 Site Reference ID/Investigator# 27482 Vienna, Austria, 1130 Site Reference ID/Investigator# 10981 Vienna, Austria, 1220 收起 <<

Cinacalcet hydrochloride 参考文献

[1]Ma JN, Owens M, et al. Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. J Pharmacol Exp Ther. 2011;337(1):275-84.

[2]Kawata T, Imanishi Y, et al. Direct in vitro evidence of the suppressive effect of cinacalcet HCl on parathyroid hormone secretion in human parathyroid cells with pathologically reduced calcium-sensing receptor levels. J Bone Miner Metab. 2006;24(4):300-6.

[3]Shalhoub V, Grisanti M, et al. In vitro studies with the calcimimetic, cinacalcet HCl, on normal human adult osteoblastic and osteoclastic cells. Crit Rev Eukaryot Gene Expr. 2003;13(2-4):89-106.

[4]Imanishi Y, Kawata T, et al. Cinacalcet HCl suppresses Cyclin D1 oncogene-derived parathyroid cell proliferation in a murine model for primary hyperparathyroidism. Calcif Tissue Int. 2011;89(1):29-35.

[5]Colloton M, Shatzen E, et al. Cinacalcet HCl attenuates parathyroid hyperplasia in a rat model of secondary hyperparathyroidism. Kidney Int. 2005 Feb;67(2):467-76.

[6]Cinacalcet HCl

Cinacalcet hydrochloride 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.69mL

2.54mL

1.27mL

25.39mL

5.08mL

2.54mL

Cinacalcet hydrochloride 技术信息

CAS号364782-34-3
分子式C22H23ClF3N
分子量 393.873
别名 AMG-073 hydrochloride;Cinacalcet (hydrochloride);Mimpara;KRN 1493;AMG 073;Cinacalcet HCl
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 50 mg/mL(126.94 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.54 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方

Tags: Cinacalcet hydrochloride | AMG-073 hydrochloride;Cinacalcet (hydrochloride);Mimpara;KRN 1493;AMG 073;Cinacalcet HCl | CaSR | AmBeed-信号通路专用抑制剂 | Cinacalcet hydrochloride 纯度/质量文件 | Cinacalcet hydrochloride 亚型比较 | Cinacalcet hydrochloride 生物活性 | Cinacalcet hydrochloride 动物研究 | Cinacalcet hydrochloride 临床数据 | Cinacalcet hydrochloride 参考文献 | Cinacalcet hydrochloride 实验方案 | Cinacalcet hydrochloride 技术信息

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