2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Cephaeline dihydrochloride

Cephaeline (dihydrochloride)  (Synonyms: (-)-Cephaeline (dihydrochloride); NSC 32944; セファエリン二塩酸塩)

製品番号: HY-N2260 純度: 99.67%
COA 取扱説明書 Technical Support

Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.

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CAS 番号 : 5853-29-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 142 在庫あり
Solution
10 mM * 1 mL in DMSO USD 142 在庫あり
Solid
5 mg $120 在庫あり
10 mg $180 在庫あり
25 mg $360 在庫あり
50 mg $580 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Cephaeline dihydrochloride:

Cephaeline (dihydrochloride) 関連抗体

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
Cell Migration/Invasion Assay
WB

    Cephaeline dihydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Oct;149(13):11117-11133.  [Abstract]

    MDA-MB-231 and MCF-7 cells were treated with different dose of Cephaeline (0.1, 0.5, 1, 5, 10 μM) and cell viability were calculated by Cell Counting Kit-8.

    Cephaeline dihydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Oct;149(13):11117-11133.  [Abstract]

    Representative images of cell scratch-wound healing test taken by a microscope at × 100 magnification treated with Cephaeline (0.2, 0.4 μM).

    Cephaeline dihydrochloride purchased from MedChemExpress. Usage Cited in: J Cancer Res Clin Oncol. 2023 Oct;149(13):11117-11133.  [Abstract]

    Representative western blots for PI3K/AKT signal pathway and HIF-1α under different doses of Cephaeline (0.1, 0.2, 0.3, 0.4, 0.5 μM).

    Cytochrome P450 アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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    製品説明

    Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.

    IC50 & Target

    CYP2

     

    体外実験

    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 1000 μM, 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 355 μM for CYP2D6 and CYP3A4, respectively[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cephaeline (dihydrochloride) 関連抗体
    分子量

    539.53

    分子式

    C28H40Cl2N2O4
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    Cl[H].CC[C@@H](CN1CC2)[C@H](C[C@@]1([H])C3=C2C=C(OC)C(OC)=C3)C[C@]4([H])C5=CC(OC)=C(O)C=C5CCN4.Cl[H]
    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
    溶剤 & 溶解度
    体外: 

    DMSO : 250 mg/mL (463.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 125 mg/mL (231.68 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8535 mL 9.2673 mL 18.5346 mL
    5 mM 0.3707 mL 1.8535 mL 3.7069 mL
    10 mM 0.1853 mL 0.9267 mL 1.8535 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

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    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (92.67 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.67%

    COA (258 KB) HNMR (227 KB) CNMR (219 KB) LCMS (99 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    Cephaeline is dissolved in methanol to give concentrations of 0.1, 1, 10, 100 μM (only theophylline-O-demethylase activity with Cephaeline; 0.0985, June 2001 679 0.985, 9.85, 98.5 μM) [1].
    Human liver microsomal protein is incubated with the selected marker substrates in the absence and presence of above concentrations of Cephaeline or Emetine (1-100 μM, only theophylline-O-demethylase activity with Cephaeline; 0.0985—98.5 μM, 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 32 μM; testosterone 45, 90 and 180u M) and using several inhibitor concentrations of 10, 50, and 100 μM. 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[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.8535 mL 9.2673 mL 18.5346 mL 46.3366 mL
    5 mM 0.3707 mL 1.8535 mL 3.7069 mL 9.2673 mL
    10 mM 0.1853 mL 0.9267 mL 1.8535 mL 4.6337 mL
    15 mM 0.1236 mL 0.6178 mL 1.2356 mL 3.0891 mL
    20 mM 0.0927 mL 0.4634 mL 0.9267 mL 2.3168 mL
    25 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8535 mL
    30 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5446 mL
    40 mM 0.0463 mL 0.2317 mL 0.4634 mL 1.1584 mL
    50 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9267 mL
    60 mM 0.0309 mL 0.1545 mL 0.3089 mL 0.7723 mL
    80 mM 0.0232 mL 0.1158 mL 0.2317 mL 0.5792 mL
    100 mM 0.0185 mL 0.0927 mL 0.1853 mL 0.4634 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Cephaeline dihydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Cephaeline5853-29-2(-)-Cephaeline NSC 32944NSC32944NSC 32944NSC-32944Cytochrome P450CYPsInhibitorinhibitorinhibit

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