| 中文名称: | Cephaeline dihydrochloride | ||||
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| 英文名称: | Cephaeline dihydrochloride | ||||
| 别名: | Cephaeline dihydrochloride (-)-Cephaelinedi hydrochloride;NSC32944 | ||||
| CAS No: | 5853-29-2 | 分子式: | C28H40Cl2N2O4 | 分子量: | 539.53 |
| CAS No: | 5853-29-2 | ||||
| 分子式: | C28H40Cl2N2O4 | ||||
| 分子量: | 539.53 | ||||
基本信息
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产品编号： |
C11231 |
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产品名称： |
Cephaeline dihydrochloride |
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CAS: |
5853-29-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
539.53 |
-20℃ |
一个月 |
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化学名： |
(-)-Cephaelinedi hydrochloride;NSC32944 |
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Solubility (25°C)： |
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体外:
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DMSO |
250mg/mL (463.37mM; Need ultrasonic) |
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Ethanol |
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Water |
250mg/mL (463.37mM; Need ultrasonic) |
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体内(现配现用): |
1.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08mg/mL (3.86mM); Clear solution |
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此⽅案可获得 ≥ 2.08mg/mL (3.86mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。 |
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2.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility: ≥ 2.08mg/mL (3.86mM); Clear solution |
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此⽅案可获得 ≥ 2.08mg/mL (3.86mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以 1mL ⼯作液为例，取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，混合均匀。 |
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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 |
1.8535mL |
9.2673mL |
18.5346mL |
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5mM |
0.3707mL |
1.8535mL |
3.7069mL |
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10mM |
0.1853mL |
0.9267mL |
1.8535mL |
生物活性
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产品描述 |
一种选择性的CYP2D6抑制剂。 |
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靶点 |
IC50: 121μM (CYP2D6) Ki: 54μM (CYP2D6) |
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体外研究 |
CYP2D6 reveals the highest metabolic activity for the generation of 9-O-demethylEmetine, whereas this enzyme also shows a significant metabolic activity for the generation of Cephaeline. The IC50s of Cephaeline against CYP2C9, CYP2D6 and CYP3A4 is over 1000, 121 and 1000μM, respectively. Further experiments are performed to determine inhibition constants (Ki ) for Cephaeline on the CYP2D6 and CYP3A4 activities Graphic analysis of Dixon plots at various Cephaeline concentrations for each of the two CYP enzyme assays yield Kis of 54 and 355μM for CYP2D6 and CYP3A4, respectively |
推荐实验方法(仅供参考)
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Kinase Assay |
Cephaeline is dissolved in methanol to give concentrations of 0.1, 1, 10, 100μM (only theophylline-O-demethylase activity with Cephaeline; 0.0985, June 2001 679 0.985, 9.85, 98.5μM). Human liver microsomal protein is incubated with the selected marker substrates in the absence and presence of above concentrations of Cephaeline or Emetine (1-100μM, only theophylline-O-demethylase activity with Cephaeline; 0.0985—98.5μM, final concentration). Incubation conditions are chosen such that the product formation is linear with respect to both incubation times and protein concentrations, with substrate concentrations being at or below the Km for each enzyme. The effects of furafylline, sulphaphenazole, tranylcypromine, quinidine, and ketoconazole, selective inhibitors of CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, respectively, are also determined in the same microsomal samples to provide comparisons with inhibitory potentials (IC50) of Cephaeline and Emetine towards the individual CYP form. The Ki s for Cephaeline and Emetine are determined by using the same pooled microsomal sample. This is achieved by varying the initial substrate concentrations (bufuralol 8, 16 and 32μM; testosterone 45, 90 and 180uM) and using several inhibitor concentrations of 10, 50, and 100μM. The Kis are estimated by graphic analysis of Dixon plots. These values are subsequently used as initial estimates for the nonlinear least-squares regression analysis |
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 )
