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

Cephaeline dihydrochloride  (Synonyms: (-)-Cephaeline dihydrochloride; NSC 32944)

Cat. No.: HY-N2260 Purity: 99.84%
COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

Cephaeline dihydrochloride Chemical Structure

Cephaeline dihydrochloride Chemical Structure

CAS No. : 5853-29-2

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5 mg USD 120 In-stock
10 mg USD 180 In-stock
25 mg USD 360 In-stock
50 mg USD 580 In-stock
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Based on 1 publication(s) in Google Scholar

Cephaeline dihydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

CYP2

 

In Vitro

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 Related Antibodies
Molecular Weight

539.53

Formula

C28H40Cl2N2O4
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Solvent & Solubility
In Vitro: 

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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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).
Purity & Documentation

Purity: 99.84%

COA (258 KB) HNMR (301 KB) LCMS (256 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[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].

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

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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