Ketoconazole (Synonyms: Ketoconazol; R 41400)

Name: Ketoconazole
Brand: MedChemExpress
SKU: HY-B0105
Rating: 5.0 (29 reviews)

Cat. No.: HY-B0105 Purity: 99.57%: Data Sheet
COA

SDS
Handling Instructions
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Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

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

CAS No. : 65277-42-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	Get quote
50 g	Get quote

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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of Ketoconazole:

29 Publications Citing Use of MCE Ketoconazole

Histological Imaging/Staining

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: Ketoconazole purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Nov 28;11(48):eadw8410. [Abstract]; Ketoconazole (0.05 mg/kg per day) was administered. Representative immunofluorescence images of Aβ plaques in the piriform cortex and cA1 region of the hippocampus were obtained.

: Ketoconazole purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Nov 28;11(48):eadw8410. [Abstract]; Ketoconazole (0.05 mg/kg per day) was administered. Aβ plaque density (number of plaques per square micrometer) in the cA1 region of the hippocampus was measured.

: Ketoconazole purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Nov 28;11(48):eadw8410. [Abstract]; Ketoconazole (10 μM; 13 h). Representative Western blot of Bace-1, Mdr1, p-NFκB, NFκB, and GAPDH protein levels in the cells was shown.

: Ketoconazole purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Jul 6;14(7):402. [Abstract]; Lipid peroxidation (top) and cell viability (bottom) were assessed in the indicated cells treated with erastin (20 µM) for 24 h or ketoconazole (5 µM) for 8 h.

: Ketoconazole purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2021 Nov;42(11):1834-1846. [Abstract]; The primary mouse hepatocytes were pretreated with MG132 (10 μM) and Ketoconazole (5 μM) for 30 min, followed by cotreatment with SL010110 or metformin for 4 h. Then, the PEPCK1 protein levels were measured.

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K-Ras H-Ras N-Ras Ras

Biological Activity
Purity & Documentation
References
Customer Review

Description

Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

IC₅₀ & Target

CYP3

CYP4

In Vitro

Ketoconazole (R-41400), an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections^[1].
Ketoconazole (R-41400) also is a cytochrome P450 inhibitor^[2].
Ketoconazole (R-41400), on the antischistosomal potential of these quinolines against Schistosoma mansoni infection by evaluating parasitological, histopathological, and biochemical parameters. Mice were classified into 7 groups: uninfected untreated (I), infected untreated (II), infected treated orally with PZQ (1,000 mg/kg) (III), QN (400 mg/kg) (IV), KTZ (10 mg/kg)+QN as group IV (V), HF (400 mg/kg) (VI), and KTZ (as group V)+HF (as group VI) (VII). KTZ plus QN or HF produced more inhibition (P<0.05) in hepatic CYP450 (85.7% and 83.8%) and CYT b5 (75.5% and 73.5%) activities, respectively, than in groups treated with QN or HF alone. This was accompanied with more reduction in female (89.0% and 79.3%), total worms (81.4% and 70.3%), and eggs burden (hepatic; 83.8%, 66.0% and intestinal; 68%, 64.5%), respectively, and encountering the granulomatous reaction to parasite eggs trapped in the liver^[3].
CYP24A1 inhibitor enhances antiproliferative effects, increases systemic calcitriol exposure, and promotes the activation of caspase-independent apoptosis pathway. Ketoconazole is also a potent exosome biogenesis and/or secretion inhibitor^[4].

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.

65277-42-1

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 : 10 mg/mL (18.82 mM; ultrasonic and warming and heat to 60°C; 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
10 mM	0.1882 mL	0.9409 mL	1.8817 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.57%

Select Batch:

Data Sheet (276 KB) SDS (788 KB)

COA (251 KB) HNMR (127 KB) RP-HPLC (86 KB)

Handling Instructions (2659 KB)

References

[1]. Seif El-Din SH, et al. Effect of ketoconazole, a cytochrome P450 inhibitor, on the efficacy of quinine and halofantrine against Schistosoma mansoni in mice. Korean J Parasitol. 2013 Apr;51(2):165-75. [Content Brief]

[2]. Eil C. Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24(8):367-70. [Content Brief]

[3]. Muindi JR et al. CYP24A1 inhibition enhances the antitumor activity of calcitriol. Endocrinology. 2010 Sep;151(9):4301-12. [Content Brief]

[4]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. [Content Brief]

Complete Stock Solution Preparation Table

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

Ketoconazole 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:

Ketoconazole65277-42-1Ketoconazol R 41400R41400R 41400R-41400FungalCytochrome P450RasBacterialCYPsInhibitorinhibitorinhibit

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Ketoconazole (Synonyms: Ketoconazol; R 41400)

Customer Review

Other Forms of Ketoconazole:

Ketoconazole Related Antibodies

29 Publications Citing Use of MCE Ketoconazole

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Cytochrome P450 Isoform Specific Products:

View All Ras Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Ketoconazole Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ketoconazole Related Classifications

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Your Recently Viewed Products:

Customer Review

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