产品说明书

Cinacalcet

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Chemical Structure| 226256-56-0 同义名 : AMG 073;Sensipar;Cin
CAS号 : 226256-56-0
货号 : A621347
分子式 : C22H22F3N
纯度 : 98%
分子量 : 357.412
MDL号 : MFCD09840270
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

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：
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].
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 <<
实验方案
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
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.