Cat. No.: HY-B0105

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Ketoconazole

(Synonyms: Ketoconazol; R 41400)

30 Cited Publications

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Based on 30 publication(s) in Google Scholar

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

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Pureté: 99.57%
CAS No.: 65277-42-1
Formule: C₂₆H₂₈Cl₂N₄O₄
Masse moléculaire:531.43

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ketoconazole Chemical Structure

CAS No.: 65277-42-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Essai clinique
Chemical Information
Publications (30)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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

IC₅₀ & Target

CYP3

CYP4

Voir tous les produits spécifiques à Isoform Cytochrome P450 :

Voir tous les produits spécifiques à Isoform Ras :

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 65277-42-1
Appearance Solid
Masse moléculaire 531.43
Formule C₂₆H₂₈Cl₂N₄O₄
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
Synonyms

Ketoconazol; R 41400
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (30)

All Histological Imaging/StainingCell Proliferation/Viability AssayIn Vivo Efficacy StudyWB

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Journal Impact Factor

Cell

Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]

2025 May 29;188(11):3065-3080.e21. PMID: 40393457
Adv Sci (Weinh)

Mitochondrial-Targeted CS@KET/P780 Nanoplatform for Site-Specific Delivery and High-Efficiency Cancer Immunotherapy in Hepatocellular Carcinoma. [Abstract]

2024 Apr;11(14):e2308027. PMID: 38308137
Sci Adv

Gut microbial-derived indole-3-propionate improves cognitive function in Alzheimer's disease. [Abstract]

2025 Nov 28;11(48):eadw8410. PMID: 41313780

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.
Cell Death Dis

USP11-mediated LSH deubiquitination inhibits ferroptosis in colorectal cancer through epigenetic activation of CYP24A1. [Abstract]

2023 Jul 6;14(7):402. PMID: 37414755

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.
Acta Pharmacol Sin

SL010110, a lead compound, inhibits gluconeogenesis via SIRT2-p300-mediated PEPCK1 degradation and improves glucose homeostasis in diabetic mice. [Abstract]

2021 Nov;42(11):1834-1846. PMID: 33574568

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.
Environ Int

A potential biomarker of isofenphos-methyl in humans: A chiral view. [Abstract]

2019 Jun:127:694-703. PMID: 30991225
Anal Chem

A Computational Integration Strategy Driven by Chemical Similarity Uncovers Comprehensive Metabolic Profiles of Small Bioactive Peptides via UHPLC-HRMS for Doping Control. [Abstract]

2025 Nov 18;97(45):25158-25167. PMID: 41202118
Environ Pollut

Enantioselective metabolic mechanism and metabolism pathway of tetraconazole in human liver microsomes: In vitro and in silico study. [Abstract]

2026 May 1:396:127849. PMID: 41720237
Pharmaceutics

Plasma Protein Binding, Biostability, Metabolite Profiling, and CYP450 Phenotype of TPB15 Across Different Species: A Novel Smoothened Inhibitor for TNBC Therapy. [Abstract]

2025 Mar 26;17(4):423. PMID: 40284418
Cell Biosci

Gut microbial metabolite deoxycholic acid facilitates Th17 differentiation through modulating cholesterol biosynthesis and participates in high-fat diet-associated colonic inflammation. [Abstract]

2023 Oct 3;13(1):186. PMID: 37789469
Food Biosci

2025 Jun.
Front Microbiol

Ketoconazole induces reversible antifungal drug tolerance mediated by trisomy of chromosome R in Candida albicans. [Abstract]

2024 Jul 30:15:1450557. PMID: 39139375
Int J Mol Sci

LRRC8A Inhibition Overcomes Chemoresistance by Downregulating MRP3 and CYP3A4 in the 3D Spheroid Model of Human Breast Cancer Cells. [Abstract]

2026 Mar 13;27(6):2646. PMID: 41898509
Int Immunopharmacol

Synergistic and mechanistic effects of neogambogic acid in enhancing almonertinib sensitivity in non-small cell lung cancer. [Abstract]

2025 Jun 26:159:114878. PMID: 40412130
Molecules

Fraxinellone Induces Hepatotoxicity in Zebrafish through Oxidative Stress and the Transporters Pathway. [Abstract]

2022 Apr 20;27(9):2647. PMID: 35566003
Biochim Biophys Acta Mol Basis Dis

YY2-CYP51A1 signaling suppresses hepatocellular carcinoma progression by restraining de novo cholesterol biosynthesis. [Abstract]

2025 Mar;1871(3):167658. PMID: 39761760
ACS Infect Dis

(Heteroarylmethyl)benzoic Acids as a New Class of Bacterial Cystathionine γ-Lyase Inhibitors: Synthesis, Biological Evaluation, and Molecular Modeling. [Abstract]

2024 Jun 14;10(6):2127-2150. PMID: 38771206
Clin Exp Med

CYP51-mediated cholesterol biosynthesis is required for the proliferation of CD4+ T cells in Sjogren's syndrome. [Abstract]

2023 Sep;23(5):1691-1711. PMID: 36413274
Clin Transl Sci

Inhibition of Tacrolimus Metabolism by Cannabidiol and Its Metabolites In Vitro. [Abstract]

2025 Feb;18(2):e70152. PMID: 39921332
Cancer Res Commun

Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition. [Abstract]

2021 Nov;1(2):79-89. PMID: 34950932
Toxicol Appl Pharmacol

Bulleyaconitine A is a sensitive substrate and competitive inhibitor of CYP3A4: One of the possible explanations for clinical adverse reactions. [Abstract]

2022 Jun 15;445:116024. PMID: 35439480
Food Chem Toxicol

Clinical poisoning events involving yunaconitine may be highly correlated with metabolism-based interactions: A critical role of CYP3A4. [Abstract]

2023 Sep:179:113989. PMID: 37619830
Food Chem Toxicol

The "steric-like" inhibitory effect and mechanism of doxycycline on florfenicol metabolism: Interaction risk. [Abstract]

2022 Nov:169:113431. PMID: 36116547
Drug Test Anal

High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]

2021 Feb;13(2):283-298. PMID: 32852861
J Chromatogr B Analyt Technol Biomed Life Sci

Development and validation of a sensitive UHPLC-MS/MS analytical method for venetoclax in mouse plasma, and its application to pharmacokinetic studies. [Abstract]

2020 Sep 1:1152:122176. PMID: 32534260
Biopharm Drug Dispos

Metabolic interaction between biflavonoids in Ginkgo biloba leaves and tacrolimus. [Abstract]

2023 Apr;44(2):157-164. PMID: 36840704
Biopharm Drug Dispos

Inhibition of canalicular and sinusoidal taurocholate efflux by cholestatic drugs in human hepatoma HepaRG cells. [Abstract]

2022 Dec;43(6):265-271. PMID: 36195987
Cell Press Blue

2026 Apr 22.
Chemosphere

A proposed "steric-like effect" for the slowdown of enrofloxacin antibiotic metabolism by ciprofloxacin, and its mechanism. [Abstract]

2021 Dec:284:131347. PMID: 34323809
Research Square Preprint

2020 Dec.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Ketoconazole

30 Cited Publications

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Ketoconazole

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Publications Citing Use of MedChemExpress (MCE) Ketoconazole

Voir tous les produits spécifiques à Isoform Cytochrome P450

Voir tous les produits spécifiques à Isoform Ras

Activité biologique

Chemical Information

Publications (30)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ketoconazole Related Classifications

HY-B0105 Related Classifications