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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / CaSR / Cinacalcet/西那卡塞

Cinacalcet/西那卡塞 {[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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Cinacalcet/西那卡塞 化学结构 CAS号：226256-56-0
Cinacalcet/西那卡塞 化学结构
CAS号：226256-56-0
Cinacalcet/西那卡塞 3D分子结构
CAS号：226256-56-0
Cinacalcet/西那卡塞 化学结构 CAS号：226256-56-0
Cinacalcet/西那卡塞 3D分子结构 CAS号：226256-56-0
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Cinacalcet/西那卡塞 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/西那卡塞 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/西那卡塞 细胞实验

Cell Line
Concentration Treated Time Description References
Enterococcus faecalis (LRE 16C352) 12.5 mg/mL 16 hours Cinacalcet at concentrations above 12.5 mg/mL could completely inhibit growth of planktonic cells iScience. 2023 Mar 11;26(4):106378.
Enterococcus faecalis (E. faecalis 16C51) 12.5 mg/mL 16 hours Cinacalcet at concentrations above 12.5 mg/mL could completely inhibit growth of planktonic cells iScience. 2023 Mar 11;26(4):106378.
Staphylococcus aureus (MRSA YUSA145) 12.5 mg/mL 16 hours Cinacalcet at concentrations above 12.5 mg/mL could completely inhibit growth of planktonic cells iScience. 2023 Mar 11;26(4):106378.
Staphylococcus aureus (MSSA CHS101) 12.5 mg/mL 16 hours Cinacalcet at concentrations above 12.5 mg/mL could completely inhibit growth of planktonic cells iScience. 2023 Mar 11;26(4):106378.
Osteoclasts 400 nM 18 hours Cinacalcet significantly reduced the bone resorption area and increased Wnt10b expression and release from osteoclasts. Int J Mol Sci. 2019 Jun 8;20(11):2800.
MDCK cells 30 µM 20 minutes Cinacalcet inhibited forskolin-induced cAMP elevation by 60%, and its effect was completely reversed by IBMX Transl Res. 2024 Mar;265:17-25.
MDCK cells 30 µM 20 minutes Cinacalcet inhibited forskolin-induced Cl− secretion and CFTR activity, reducing short-circuit current changes by ~70% Transl Res. 2024 Mar;265:17-25.
Human intestinal T84 cells 30 µM 20 minutes Cinacalcet pretreatment inhibited all 3 components of forskolin and cholera toxin-induced secretory short-circuit currents (Isc) (CFTR, Clc-2, and K+ channels) by ∼75%. Transl Res. 2024 Jan;263:45-52.
HBE cells 30 µM 20 minutes Cinacalcet pretreatment significantly inhibited CFTR-mediated Cl- secretion but had no significant effect on ENaC or CaCC activities. JCI Insight. 2021 Feb 22;6(4):e146823.
FRT cells 30 µM 20 minutes Cinacalcet pretreatment did not affect CFTR-mediated Cl- conductance, indicating its inhibitory effect on CFTR is dependent on CaSR activation. JCI Insight. 2021 Feb 22;6(4):e146823.
T84 cells 10 µM and 30 µM 20 minutes Cinacalcet significantly inhibited forskolin-induced Cl- secretion, reducing ISC increase by approximately 50% and 85%, respectively. JCI Insight. 2021 Feb 22;6(4):e146823.
HEK293 cells 10 nM 20 minutes To evaluate the effect of Cinacalcet on signaling in Gα11 Asp195Gly mutant cells, results showed that 10 nM Cinacalcet corrected the signaling abnormalities in mutant cells. JCI Insight. 2017 Oct 19;2(20):e96540.
Bone marrow-derived macrophages (BMDMs) 0.1, 1, 5 µM 24 hours Cinacalcet significantly reduced the TNFα-induced mRNA expression and secretion levels of inflammatory cytokines IL-1β and IL-6. Front Pharmacol. 2021 Nov 22;12:735194.
RAW264.7 cells 0.1, 1, 5 µM 24 hours Cinacalcet significantly reduced the TNFα-induced mRNA expression and secretion levels of inflammatory cytokines IL-1β and IL-6. Front Pharmacol. 2021 Nov 22;12:735194.
HEK293 cells 100 nM 30 minutes To evaluate the effect of Cinacalcet on intracellular calcium signaling in HEK293 cells expressing wild-type and mutant CaSR, results showed that Cinacalcet could correct the abnormal intracellular calcium signaling caused by Ile555Thr mutation. J Clin Endocrinol Metab. 2024 Jan 18;109(2):549-556.
Human primary ADPKD cells 3 µM 6 days Cinacalcet inhibited forskolin-induced cyst enlargement by 60% and reduced cell proliferation Transl Res. 2024 Mar;265:17-25.
MDCK cells 1-10 µM 6 days Cinacalcet concentration-dependently reduced cell proliferation, cyst formation and cyst enlargement by up to 50% without affecting cell viability Transl Res. 2024 Mar;265:17-25.
Cells expressing the calcium-sensing receptor and AP2-sigma mutants 10 nM Corrected the abnormal intracellular calcium signaling and MAPK responses to extracellular calcium N Engl J Med. 2016 Apr 7;374(14):1396-1398.

Cinacalcet/西那卡塞 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice DSS-induced colitis model Oral gavage 0.1, 1, 10 mg/kg Daily administration until the end of the experiment Cinacalcet significantly reduced the disease activity index score, prevented colon shortening, diminished inflammatory cell infiltration, and protected the structural integrity of the intestinal wall. Additionally, Cinacalcet reduced the production of inflammatory cytokines TNFα, IL-1β, and IL-6 in the colon and sera of mice with DSS-induced colitis. Front Pharmacol. 2021 Nov 22;12:735194.
Mice Intestinal closed loop models of cholera and traveler’s diarrhea Intraperitoneal injection 1, 10 and 30 mg/kg Single dose, lasting 3 hours Cinacalcet at 30 mg/kg significantly inhibited intestinal fluid accumulation induced by cholera toxin and STa toxin, reducing fluid accumulation by approximately 75% and 60%, respectively. JCI Insight. 2021 Feb 22;6(4):e146823.
Mice (BALB/c and C57BL/6J) Pneumonia infection model and deep-seated infection model Intraperitoneal injection 10 mg/kg (pneumonia model) and 40 mg/kg (deep-seated infection model) Every 24 hours for 2 days Cinacalcet exhibited high anti-infective efficacy in vivo, comparable to vancomycin iScience. 2023 Mar 11;26(4):106378.
C57BL/6 mice 5/6 nephrectomy CKD model Oral gavage 10 mg/kg/day Once daily for 4 weeks Cinacalcet significantly decreased serum PTH levels, reduced cortical porosity, and improved bone strength and stiffness. Int J Mol Sci. 2019 Jun 8;20(11):2800.
Mice ADPKD mouse model Subcutaneous injection 20 mg/kg/day Once daily for 7 days Cinacalcet treatment reduced renal cyst enlargement by 20%, decreased kidney/body weight ratio and serum BUN Transl Res. 2024 Mar;265:17-25.
Mice Cholera toxin-induced secretory diarrhea model Oral 30 mg/kg Single dose, evaluated at 20 hours Cinacalcet inhibited forskolin-induced secretory Isc by ～60% in wild-type mice and had no antisecretory effect in intestinal epithelia-specific Casr knockout mice. In the suckling mouse model of cholera induced by oral cholera toxin, a single oral dose of cinacalcet reduced intestinal fluid accumulation by ～55% at 20 hours. Transl Res. 2024 Jan;263:45-52.
Mice Gna11+/195G and Gna11195G/195G mice Oral 30 mg/kg Single dose, plasma samples collected at 0, 1, 2, 4, 6, and 24 hours post-dose To evaluate the effect of Cinacalcet on hypercalcemia and PTH levels in Gna11 mutant mice, results showed that Cinacalcet significantly reduced plasma calcium and PTH concentrations. JCI Insight. 2017 Oct 19;2(20):e96540.

Cinacalcet/西那卡塞 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/西那卡塞 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/西那卡塞 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/西那卡塞 技术信息

CAS号226256-56-0
分子式C22H22F3N
分子量 357.41
SMILES Code FC(C1=CC(CCCN[C@@H](C2=C3C=CC=CC3=CC=C2)C)=CC=C1)(F)F
MDL No. MFCD09840270
别名 AMG 073; Sensipar; Cin
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Cinacalcet | AMG 073;Sensipar;Cin | CaSR | AmBeed-信号通路专用抑制剂 | Cinacalcet/西那卡塞 纯度/质量文件 | Cinacalcet/西那卡塞 亚型比较 | Cinacalcet/西那卡塞 生物活性 | Cinacalcet/西那卡塞 临床数据 | Cinacalcet/西那卡塞 参考文献 | Cinacalcet/西那卡塞 实验方案 | Cinacalcet/西那卡塞 技术信息

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