计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Cinacalcet Hydrochloride is a type II calcimimetic agent which controls calcium levels in cells by allosteric activation of CaSR (calcium sensing receptors). Studies show that Cinacalcet Hydrochloride affects cell proliferation in CHO cells transfected with CaSRs. In addition, it is known that Cinacalcet Hydrochloride inhibits the secretion of the parathyroid hormone (PTH). These studies sμggest that Cinacalcet Hydrochloride in instrumental in increasing the cytoplasmic concentration of Ca2+. Furthermore, Cinacalcet Hydrochloride is an analog of NPS R-568 which contains a much better metabolic profile.An allosteric activator of CaSR
Information
Cinacalcet (AMG-073) HCl Cinacalcet (AMG-073) HCl represents a new class of compounds for the treatment of hyperparathyroidism.
In vitro
AMG-073 represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium. AMG-073 has potential advantages as a therapy for secondary hyperparathyroidism because it mimics the effects of extracellular calcium to suppress PTH secretion, even in the presence of hyperphosphatemia, without the risk of causing hypercalcemia and/or hyperphosphatemia. AMG-073 produces a concentration-dependent increase in cytoplasmic calcium in human embryonic kidney cells expressing the CaSR. In bovine parathyroid cells and a buffer containing calcium 0.5 mM, AMG 073 (3 nM – 1 μM) produces a concentration-dependent decrease in PTH levels with IC50 of 27 nM.
In vivo
AMG-073 orally administrated to normal rats at dose of 1, 3, 10, and 30 mg/kg in 20% sulfobutyl ether β-cyclodextrin sodium produces a significant dose-dependent reduction in PTH levels for 1 to 4 hours after administration. At 8 hours, the 10- and 30-mg/kg doses of AMG-073 produces significant reductions in PTH levels compared with controls that disappears by 24 hours. Significant dose-dependent reduction in serum calcium levels are observed at 4, 8, and 24 hours after oral administration of AMG-073 3, 10, and 30 mg/kg, respectively. A transient reduction in serum phosphorus levels is observed only with the highest dose of AMG-073. In addition, increased calcitonin levels that paralleled PTH suppression are observed with AMG-073 40 mg/kg in rats. As in normal rats, a rapid dose-dependent reduction in PTH and calcium levels is observed in 5 of 6 nephrectomized rats after oral administration of AMG-073. In addition, oral AMG-073 at 5 and 10 mg/kg for 4 weeks significantly reduces parathyroid weight compared with controls.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
别名
西那卡塞(AMG-073)盐酸盐
英文别名
(R)-N-(1-(naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine hydrochloride
规格或纯度
10mM in DMSO
英文名称
Cinacalcet (AMG-073) HCl
生化机理
盐酸西那卡西特（AMG-073）是治疗甲状旁腺功能亢进症的一类新型化合物。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
正变构调节剂
作用机制
钙传感受体正异位调节剂
名称和识别符
EC号
620-490-5
分子类型
小分子
Isomeric SMILES
C[C@H](C1=CC=CC2=CC=CC=C21)NCCCC3=CC(=CC=C3)C(F)(F)F.Cl
PubChem CID
分子量
393.87
技术文档
高级数据
关联靶点（人）
CASR
Tclin
细胞外钙敏感受体(Extracellular calcium-sensing receptor)
(1 活性数据)
安全和危险性（GHS）
信号词
Danger
危险声明
H319: 引起严重眼睛刺激
H373: 通过长时间或反复暴露对器官造成损害
H412: 对水生生物有害并具有长期持续影响
H413: 可能对水生生物造成长期的有害影响
H302: 吞食有害
H318: 造成严重的眼睛损伤
H317: 可能引起皮肤过敏反应
H312: 皮肤接触有害
H400: 对水生生物有剧毒
H410: 对水生生物有剧毒并具有长期持续影响
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P273: 避免释放到环境中。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P302+P352: 如皮肤沾染：用水充分清洗。
P321: 特殊处理（请参阅此标签上的...）。
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P272: 被污染的工作服不允许离开工作场所
P333+P313: 如发生皮肤刺激或皮疹：求医/就诊。
P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。
P391: 收集溢出物
P330: 漱口
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P301+P317: 如果被吞咽：请寻求医疗帮助。
P305+P354+P338: 如果进入眼睛：立即用水冲洗几分钟。取下隐形眼镜（如果有的话），并且操作简单。继续冲洗。
P317: 寻求紧急医疗救助。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
P319: 如果你感到不适，请寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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危险品化学品经营许可证（带存储）