Cephaeline dihydrochloride  ≥98%(HPLC),分析标准品

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包装规格:5mg in glass bottle
产品描述:基本信息 产品编号: C11231 产品名称: Cephaeline dihydrochloride CAS: 5853-29-2   储存条件 粉末 -20℃ 四年     分子式: C28H40Cl2N2O4 溶于液体 -80℃ 两年 分子量 539.53 -20℃ 一个月 化学名:  (-)-Cephaelinedi hydrochloride;NSC32944 Solubility (25°C):   体外:   DMSO 250mg/mL (463.37mM; Need ultrasonic) Ethanol   Water 250mg/mL (463.37mM; Need ultrasonic) 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 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。 2.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.08mg/mL (3.86mM); Clear solution 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。 <1mg/ml表示微溶或不溶。 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。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.8535mL 9.2673mL 18.5346mL 5mM 0.3707mL 1.8535mL 3.7069mL 10mM 0.1853mL 0.9267mL 1.8535mL   生物活性 产品描述 一种选择性的CYP2D6抑制剂。 靶点 IC50: 121μM (CYP2D6) Ki: 54μM (CYP2D6) 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) 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
保存条件:-20℃