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

Cinacalcet HCl/盐酸西那卡塞 {[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 HCl/盐酸西那卡塞 化学结构 CAS号：364782-34-3
Cinacalcet HCl/盐酸西那卡塞 化学结构
CAS号：364782-34-3
Cinacalcet HCl/盐酸西那卡塞 3D分子结构
CAS号：364782-34-3
Cinacalcet HCl/盐酸西那卡塞 化学结构 CAS号：364782-34-3
Cinacalcet HCl/盐酸西那卡塞 3D分子结构 CAS号：364782-34-3
规格 价格 会员价 库存 数量
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Cinacalcet HCl/盐酸西那卡塞 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 HCl/盐酸西那卡塞 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 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 HCl/盐酸西那卡塞 细胞实验

Cell Line
Concentration Treated Time Description References
T84 cells 30 µM 20 minutes Cinacalcet pretreatment inhibited all 3 components of forskolin and cholera toxin-induced secretory I sc by ∼75%. Transl Res. 2024 Jan;263:45-52.
MDCK cells 30 µM 20 minutes Cinacalcet inhibited forskolin-induced cAMP elevation, and its effect was completely reversed by PDE inhibitor IBMX Transl Res. 2024 Mar;265:17-25.
HEK293 cells 10 nM 20 minutes Cinacalcet normalized the signaling responses of Gly195 mutant Gα11 protein, reducing the EC50 from 3.39 mM to 2.70 mM, which was indistinguishable from untreated WT cells. JCI Insight. 2017 Oct 19;2(20):e96540.
T84 cells 10 µM and 30 µM 20 minutes Cinacalcet significantly inhibited forskolin-induced Cl- secretion, primarily through indirect inhibition of CFTR-mediated Cl- secretion following activation of CaSR and downstream phospholipase C and phosphodiesterases. JCI Insight. 2021 Feb 22;6(4):e146823.
FRT cells 30 µM 20 minutes Cinacalcet did not affect CFTR-mediated Cl- conductance in FRT cells, indicating that its inhibitory effect is dependent on CaSR activation. JCI Insight. 2021 Feb 22;6(4):e146823.
HBE cells 30 µM 20 minutes Cinacalcet significantly inhibited CFTR-mediated Cl- secretion in HBE cells but had no significant effect on ENaC or CaCC activities. JCI Insight. 2021 Feb 22;6(4):e146823.
HEK293 cells 100 nM 30 minutes Cinacalcet rectified the abnormal intracellular calcium signaling of Ile555Thr CaSR protein, restoring its response to changes in extracellular calcium concentrations. J Clin Endocrinol Metab. 2024 Jan 18;109(2):549-556.
MDCK cells 10 µM 6 days Cinacalcet concentration-dependently reduced cyst growth in MDCK cells by up to 50% Transl Res. 2024 Mar;265:17-25.
Human ADPKD cells 3 µM 6 days Cinacalcet treatment inhibited forskolin-induced cyst enlargement in human ADPKD cells by 60% Transl Res. 2024 Mar;265:17-25.

Cinacalcet HCl/盐酸西那卡塞 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Intestinal closed loop models of cholera and traveler’s diarrhea Intraperitoneal injection 1 mg/kg, 10 mg/kg, and 30 mg/kg Single dose, lasting 3 hours Cinacalcet significantly reduced cholera toxin- and STa toxin-induced intestinal fluid accumulation, primarily through inhibition of CFTR-mediated secretion and stimulation of NHE3-mediated absorption. JCI Insight. 2021 Feb 22;6(4):e146823.
Mice ADPKD mouse model Subcutaneous injection 20 mg/kg/day Once daily for 7 days Cinacalcet treatment reduced renal cyst index in the ADPKD mouse model by 20% Transl Res. 2024 Mar;265:17-25.
Mice Gna11+/195G and Gna11195G/195G mice Oral 30 mg/kg Single dose, monitored for 24 hours Cinacalcet significantly reduced plasma calcium and PTH concentrations in Gna11+/195G and Gna11195G/195G mice, with plasma calcium significantly reduced between 2-6 hours after dose and PTH significantly reduced at 1 hour after dose, returning to baseline by 4-6 hours. JCI Insight. 2017 Oct 19;2(20):e96540.
Mice Wild type mice 30 μM 20 minutes Cinacalcet pretreatment reduced forskolin-induced secretory Isc by 55%. Transl Res. 2024 Jan;263:45-52.

Cinacalcet HCl/盐酸西那卡塞 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 HCl/盐酸西那卡塞 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
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 HCl/盐酸西那卡塞 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 HCl/盐酸西那卡塞 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.69mL

2.54mL

1.27mL

25.39mL

5.08mL

2.54mL

Cinacalcet HCl/盐酸西那卡塞 技术信息

CAS号364782-34-3
分子式C22H23ClF3N
分子量 393.87
SMILES Code FC(C1=CC(CCCN[C@@H](C2=C3C=CC=CC3=CC=C2)C)=CC=C1)(F)F.[H]Cl
MDL No. MFCD08067750
别名 AMG-073 hydrochloride; Cinacalcet (hydrochloride); Mimpara; KRN 1493; AMG 073; Cinacalcet HCl
运输蓝冰
InChI Key QANQWUQOEJZMLL-PKLMIRHRSA-N
Pubchem ID 156418
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

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

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 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 HCl/盐酸西那卡塞 纯度/质量文件 | Cinacalcet HCl/盐酸西那卡塞 亚型比较 | Cinacalcet HCl/盐酸西那卡塞 生物活性 | Cinacalcet HCl/盐酸西那卡塞 动物研究 | Cinacalcet HCl/盐酸西那卡塞 临床数据 | Cinacalcet HCl/盐酸西那卡塞 参考文献 | Cinacalcet HCl/盐酸西那卡塞 实验方案 | Cinacalcet HCl/盐酸西那卡塞 技术信息

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