所有图片(1)
别名:
AMG 073盐酸盐, KRN 1493盐酸盐, N-[1-（R）-（-）-（1-萘基）乙基]-3-[3（三氟甲基）苯基]丙-1-氨基丙烷盐酸盐, NPS 1493盐酸盐
经验公式（希尔记法）:
C22H22F3N·HCl
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检测方案
≥98% (HPLC)
形式
powder
旋光性
[α]/D -24 to -32°, c = 0.5 in methanol
储存条件
desiccated
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
InChI
1S/C22H22F3N.ClH/c1-16(20-13-5-10-18-9-2-3-12-21(18)20)26-14-6-8-17-7-4-11-19(15-17)22(23,24)25;/h2-5,7,9-13,15-16,26H,6,8,14H2,1H3;1H/t16-;/m1./s1
InChI key
QANQWUQOEJZMLL-PKLMIRHRSA-N
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应用
Cinacalcet hydrochloride has been used:
- to stimulate calcium-sensing receptor (CaSR) in thick ascending limb (TAL) of the male Sprague-Dawley rats to study the effect of altered claudins levels on calciuria and magnesiuria in metabolic acidosis
- as a calcimimetic positive allosteric modulator (PAM) of CaSR to determine the structural rearrangements of human CaSR upon activation
- as a calcium-sensing receptor (CaSR) agonist to study the effect of CaSR on tumor cell proliferation in lung adenocarcinoma (LUAD) cell line
生化/生理作用
西那卡塞是钙敏感受体（CaSR）的正向别构调节剂，可作为拟钙剂。 它增加了钙敏感受体对细胞外钙的敏感性，导致血清钙水平降低。
Studies show that oral administration of cinacalcet hydrochloride aids in treating secondary hyperparathyroidism in patients with chronic kidney disease on dialysis. It may also be a potential therapeutic to treat hypercalcemia in patients with parathyroid carcinoma.
警示用语：
Danger
危险分类
Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Dam. 1 - Skin Corr. 1A - Skin Sens. 1B - STOT RE 2
靶器官
eye - retina
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
监管及禁止进口产品
Gamal A E Mostafa et al.
Profiles of drug substances, excipients, and related methodology, 42, 1-90 (2017-04-23)
Cinacalcet hydrochloride is a calcimimetic agent that increases the sensitivity to the extracellular calcium of the calcium-sensing receptors of the parathyroid gland which regulates parathyroid hormone secretion. This comprehensive profile on cinacalcet hydrochloride starts with a description: nomenclature, formulae, chemical
Clinical and Practical Use of Calcimimetics in Dialysis Patients With Secondary Hyperparathyroidism.
Jordi Bover et al.
Clinical journal of the American Society of Nephrology : CJASN, 11(1), 161-174 (2015-08-01)
CKD and CKD-related mineral and bone disorders (CKD-MBDs) are associated with high cardiovascular and mortality risks. In randomized clinical trials (RCTs), no single drug intervention has been shown to reduce the high mortality risk in dialysis patients, but several robust
Yang Gao et al.
Nature, 595(7867), 455-459 (2021-07-02)
The calcium-sensing receptor (CaSR), a cell-surface sensor for Ca2+, is the master regulator of calcium homeostasis in humans and is the target of calcimimetic drugs for the treatment of parathyroid disorders1. CaSR is a family C G-protein-coupled receptor2 that functions
Cinacalcet for Symptomatic Hypercalcemia Caused by AP2S1 Mutations.
Sarah A Howles et al.
The New England journal of medicine, 374(14), 1396-1398 (2016-04-07)
Cecelia A Byrnes et al.
Pharmacotherapy, 25(5), 709-716 (2005-05-19)
Cinacalcet is the first calcimimetic drug approved by the United States Food and Drug Administration for the treatment of secondary hyperparathyroidism in patients with chronic kidney disease. A literature search, performed by using PubMed and MEDLINE from January 1997-June 2004
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