2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Levoketoconazole

Levoketoconazole  (Synonyms: (-)-Ketoconazole; (-)-Ketoconazol; (-)-R 41400)

Cat. No.: HY-B0105B Purity: 99.39%
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Levoketoconazole ((-)-Ketoconazole) is the 2S,4R enantiomer derived from racemic Ketoconazole (HY-B0105). Levoketoconazole is a potent and orally active cortisol synthesis inhibitor. Levoketoconazole inhibits key steps in cortisol and testosterone synthesis by inhibiting CYP11B1, CYP11A1, and CYP17A1. Levoketoconazole can be used for research on endogenous Cushing’s syndrome.

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

Levoketoconazole

Levoketoconazole Chemical Structure

CAS No. : 142128-57-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Levoketoconazole:

Levoketoconazole Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Levoketoconazole

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Levoketoconazole ((-)-Ketoconazole) is the 2S,4R enantiomer derived from racemic Ketoconazole (HY-B0105). Levoketoconazole is a potent and orally active cortisol synthesis inhibitor. Levoketoconazole inhibits key steps in cortisol and testosterone synthesis by inhibiting CYP11B1, CYP11A1, and CYP17A1. Levoketoconazole can be used for research on endogenous Cushing’s syndrome[1][2].

IC50 & Target[2]

CYP11B1

 

CYP11A1

 

CYP17A1

 

In Vitro

Levoketoconazole (0.05-5 µM, 24-72 h) potently suppresses cortisol production in HAC15 cells with an IC50 of 0.300 µM (72 h)[3].
Levoketoconazole (0.1-10 µM, 1-7 days) inhibits cell number (7 days IC50 = 1.05 µM) in a time- and dose-dependent manner, and also significantly inhibits ACTH secretion in corticotroph pituitary murine AtT20 cells after 3 days of treatment[3].
Levoketoconazole (5 µM, 7 days) significantly inhibits cell number after 7 days in primary human corticotroph pituitary adenoma cultures[3].

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

Levoketoconazole Related Antibodies

Cell Proliferation Assay[3]

Cell Line: murine AtT20 cells
Concentration: 0.1-10 µM
Incubation Time: 1, 3, 7 days
Result: Inhibited murine AtT20 cell number in a time- and dose-dependent manner.
Inhibited murine AtT20 cell number with an IC50 of 1.05 µM after 7 days treatment.
In Vivo

Levoketoconazole inhibits serum corticosterone in rats[3].

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

531.43

Formula

C26H28Cl2N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N1CCN(C2=CC=C(OC[C@H]3O[C@](CN4C=CN=C4)(C5=CC=C(Cl)C=C5Cl)OC3)C=C2)CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (62.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8817 mL 9.4086 mL 18.8172 mL
5 mM 0.3763 mL 1.8817 mL 3.7634 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8817 mL 9.4086 mL 18.8172 mL 47.0429 mL
5 mM 0.3763 mL 1.8817 mL 3.7634 mL 9.4086 mL
10 mM 0.1882 mL 0.9409 mL 1.8817 mL 4.7043 mL
15 mM 0.1254 mL 0.6272 mL 1.2545 mL 3.1362 mL
20 mM 0.0941 mL 0.4704 mL 0.9409 mL 2.3521 mL
25 mM 0.0753 mL 0.3763 mL 0.7527 mL 1.8817 mL
30 mM 0.0627 mL 0.3136 mL 0.6272 mL 1.5681 mL
40 mM 0.0470 mL 0.2352 mL 0.4704 mL 1.1761 mL
50 mM 0.0376 mL 0.1882 mL 0.3763 mL 0.9409 mL
60 mM 0.0314 mL 0.1568 mL 0.3136 mL 0.7840 mL
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Levoketoconazole 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:

Levoketoconazole142128-57-2(-)-Ketoconazole(-)-Ketoconazol(-)-R 41400Cytochrome P450CYPsEnantiomercortisol synthesisCushing’s syndromeInhibitorinhibitorinhibit

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