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
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
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
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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.
signalword
Danger
hcodes
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
此项目有
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
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
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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