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

货号:A621347 同义名: AMG 073;Sensipar

Cinacalcet(AMG 073)是一种口服活性、别构激动剂的钙受体(CaR),用于心血管疾病研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Cinacalcet 化学结构 CAS号:226256-56-0
Cinacalcet 化学结构
CAS号:226256-56-0
Cinacalcet 3D分子结构
CAS号:226256-56-0
Cinacalcet 化学结构 CAS号:226256-56-0
Cinacalcet 3D分子结构 CAS号:226256-56-0
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Cinacalcet 纯度/质量文件 产品仅供科研

货号:A621347 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 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 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[3]. When primary cultured human parathyroid cells were incubated with 0.5 mM extracellular Ca2+, Cinacalcet from 0 – 1000 nM additionally suppressed the secretion of parathyroid hormone at a dose-dependent manner[4]. Cinacalcet 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[5]. Oral administration of primary hyperparathyroidism mice with 1 mg/g Cinacalcet 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 compared to the untreated ones[6].

Cinacalcet 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
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 - -
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 参考文献

[1]Bushinsky DA, Laplante K, 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.

[2]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.

[3]Ma JN, Owens M, Gustafsson M, Jensen J, Tabatabaei A, Schmelzer K, Olsson R, Burstein ES. Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. J Pharmacol Exp Ther. 2011 Apr;337(1):275-84. doi: 10.1124/jpet.110.178194. Epub 2011 Jan 14. PMID: 21239511.

[4]Kawata T, Imanishi Y, Kobayashi K, Onoda N, Okuno S, Takemoto Y, Komo T, Tahara H, Wada M, Nagano N, Ishimura E, Miki T, Ishikawa T, Inaba M, Nishizawa Y. 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. doi: 10.1007/s00774-006-0687-y. PMID: 16816924.

[5]Shalhoub V, Grisanti M, Padagas J, Scully S, Rattan A, Qi M, Varnum B, Vezina C, Lacey D, Martin D. 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. doi: 10.1615/critreveukaryotgeneexpr.v13.i24.30. PMID: 14696958.

[6]Imanishi Y, Kawata T, Kenko T, Wada M, Nagano N, Miki T, Arnold A, Inaba M. Cinacalcet HCl suppresses Cyclin D1 oncogene-derived parathyroid cell proliferation in a murine model for primary hyperparathyroidism. Calcif Tissue Int. 2011 Jul;89(1):29-35. doi: 10.1007/s00223-011-9490-4. Epub 2011 May 4. PMID: 21541686.

Cinacalcet 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

13.99mL

2.80mL

1.40mL

27.98mL

5.60mL

2.80mL

Cinacalcet 技术信息

CAS号226256-56-0
分子式C22H22F3N
分子量 357.41
别名 AMG 073;Sensipar;Cin
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(293.78 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

动物实验配方
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