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Merck
CN

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

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关于此项目

经验公式(希尔记法):
C22H22F3N·HCl
化学文摘社编号:
分子量:
393.87
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
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assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -24 to -32°, c = 0.5 in methanol

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

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

Application

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

Biochem/physiol Actions

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.


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Danger

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Dam. 1 - Skin Corr. 1A - Skin Sens. 1B - STOT RE 2

target_organs

eye - retina

存储类别

8A - Combustible corrosive hazardous materials

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

涉药品监管产品

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
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
Il Hwan Oh et al.
American journal of physiology. Renal physiology, 320(3), F418-F428 (2021-02-02)
Urinary calcium and magnesium wasting is a characteristic feature of metabolic acidosis, and this study focused on the role of the thick ascending limb of Henle's loop in metabolic acidosis-induced hypercalciuria and hypermagnesiuria because thick ascending limb is an important



全球贸易项目编号

货号GTIN
SML2012-5MG04061833247884
SML2012-50MG04061835502899
SML2012-10MG04061835502882
SML2012-25MG04061833247877