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Merck
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重要文件

SML2012

Sigma-Aldrich

西那卡塞 盐酸盐

≥98% (HPLC)

同義詞:

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

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About This Item

經驗公式(希爾表示法):
C22H22F3N·HCl
CAS號碼:
分子量::
393.87
分類程式碼代碼:
12352200
NACRES:
NA.77

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

SMILES 字串

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 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

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.

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


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分析證明 (COA)

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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
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
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)
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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