SML2012
西那卡塞 盐酸盐
≥98% (HPLC)
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
方案
≥98% (HPLC)
表单
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
SMILES字符串
FC(F)(F)c1cc(ccc1)CCCN[C@H](C)c2c3c(ccc2)cccc3.Cl
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
拟钙剂；钙敏感受体（CaSR）正向别构调节剂
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
储存分类代码
8A - Combustible corrosive hazardous materials
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
涉药品监管产品
此项目有
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
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
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
Jiansha Li et al.
Frontiers in cell and developmental biology, 8, 446-446 (2020-07-17)
The effect of calcium sensing receptor (CaSR) on tumor cell proliferation has been studied in several human cancers, and great discrepancies were found in different tumors. However, the role of CaSR in lung adenocarcinomas (LUADs) is not clear. Therefore, we
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