| 中文名称: | 盐酸西那卡塞 | ||||
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| 英文名称: | Cinacalcet hydrochloride | ||||
| 别名: | 盐酸甲状旁腺激素 AMG-073 hydrochloride | ||||
| CAS No: | 364782-34-3 | 分子式: | C22H23ClF3N | 分子量: | 393.87 |
| CAS No: | 364782-34-3 | ||||
| 分子式: | C22H23ClF3N | ||||
| 分子量: | 393.87 | ||||
基本信息
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产品编号： |
C110989 |
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产品名称： |
Cinacalcet hydrochloride |
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CAS: |
364782-34-3 |
储存条件 |
粉末 |
2-8℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
393.87 |
-20℃ |
1个月 |
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化学名： |
(R)-N-(1-(Naphthalen-1-yl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine hydrochloride |
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Solubility (25°C)： |
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体外:
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DMSO |
79mg/mL (200.57mM) |
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Ethanol |
79mg/mL (200.57mM) |
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Water |
Insoluble |
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体内(现配现用): |
30% PEG400+0.5% Tween80+5% propylene glycol |
30mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.5389mL |
12.6945mL |
25.3891mL |
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5mM |
0.5078mL |
2.5389mL |
5.0778mL |
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10mM |
0.2539mL |
1.2695mL |
2.5389mL |
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50mM |
0.0508mL |
0.2539mL |
0.5078mL |
生物活性
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产品描述 |
一种可口服的 Ca receptor (CaR) 激动剂，用于心血管疾病研究。 |
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靶点 |
CaSR |
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2.8μM(EC50) |
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体外研究 |
Cinacalcet HCl代表一种新类型的用于治理甲状腺亢进的化合物，是一种拟钙剂，通过增加甲状旁腺钙敏感受体(CaR)对细胞外钙离子的敏感性而减少甲状旁腺素(PTH)的合成和分泌。Cinacalcet HCl作为一种继发性甲状旁腺功能亢进的治疗剂，具有潜在优势，因为它模拟细胞外钙离子的作用而抑制PTH分泌，即使在患有高磷血症的情况下，也不会有引起高血钙症和/或高磷血症的风险。Cinacalcet HCl在表达CaSR的人类胚肾细胞中使细胞质中钙离子产生一个浓度依赖性的升高。在牛的甲状旁腺细胞和包含钙0.5mM，AMG 073 (3nM–1μM)的缓冲液使PTH水平浓度依赖性减少IC50 为27nM。 |
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体内研究 |
Cinacalcet (5 and 10mg/kg) results in a significant reduction in parathyroid gland weight in 5/6 nephrectomy animals.In sham animals,Cinacalcet has no effect on parathyroid gland cell proliferation or parathyroid weight compared with vehicle treatment.There are no differences in serum phosphorus levels in Cinacalcet (10,5,or 1 mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6 nephrectomized animals.Cinacalcet treatment significantly reduces blood ionized calcium levels in sham animals.Cinacalcet (30mg/kg/24h) leads to a marked reduction in circulating parathyroid hormone and a modest reduction in serum Ca.Cinacalcet does not alter UCa when the GHS rats are fed the normal Ca diet but lowers UCa when they are fed the low Ca diet.Cinacalcet does not alter U supersaturation with respect to either CaOx or CaHPO4 on either diet. |
推荐实验方法(仅供参考)
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动物实验: |
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To identify apoptosis in parathyroid glands from 5/6 nephrectomized or sham rats treated with vehicle [phosphate-buffered saline (PBS)] or Cinacalcet (10mg/kg),nuclear DNA fragmentation is measured in situ using the Apoptag System.Briefly,parathyroid gland sections from animals treated with vehicle or cinacalcet HCl are digested with 20μg/mL proteinase K in 0.1 mol/L PBS at room temperature for 15 minutes and incubated with 3% hydrogen peroxide/methanol for 5 minutes to block endogenous peroxidase. Sections are incubated for 1 hour at 37℃ with terminal deoxynucleotidyl transferase (TdT) to label exposed 3′-OH DNA ends with digoxigenin-tagged nucleotides.Digoxigenin-labeled DNA is detected by the immunoperoxidase method.Sections are developed with 3,3′-diaminobenzidine (DAB),and the nuclei of apoptotic cells are stained brown.The specificity for apoptosis is verified by negative staining when distilled water is substituted for TdT. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
