Cephaeline dihydrochloride
Based on 2 publication(s) in Google Scholar
Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 5853-29-2
- Formula: C28H40Cl2N2O4
- Molecular Weight:539.53
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Storage:
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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Cephaeline dihydrochloride
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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WB
Biological Activity
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CYP2 |
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.
Chemical Information
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CAS No. 5853-29-2
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Appearance Solid
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Molecular Weight 539.53
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Formula C28H40Cl2N2O4
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Color White to off-white
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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]
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Synonyms
(-)-Cephaeline dihydrochloride; NSC 32944
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Publications (2)
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Journal Impact Factor
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Most Recent
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J Cancer Res Clin Oncol
Prognostic value of amino acid metabolism-related gene expression in invasive breast carcinoma. [Abstract]2023 Oct;149(13):11117-11133. PMID: 37340191
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).
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Daru
2026 Jun 19;34(2):38. PMID: 42319734
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (92.67 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
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) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
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 |
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| 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.
Cephaeline dihydrochloride Related Classifications
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