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化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D -24 to -32°, c = 0.5 in methanol
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
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 密鑰
QANQWUQOEJZMLL-PKLMIRHRSA-N
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應用
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.
訊號詞
Danger
危險分類
Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Dam. 1 - Skin Corr. 1A - Skin Sens. 1B - STOT RE 2
標靶器官
eye - retina
儲存類別代碼
8A - Combustible corrosive hazardous materials
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
其他客户在看
Clinical and Practical Use of Calcimimetics in Dialysis Patients With Secondary Hyperparathyroidism.
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
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
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
Cinacalcet for Symptomatic Hypercalcemia Caused by AP2S1 Mutations.
The New England journal of medicine, 374(14), 1396-1398 (2016-04-07)
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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