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Ketoconazole

Catalog No. T0679 CAS 65277-42-1

Synonyms: R-41400, Xolegel, (±)-Ketoconazol, Extina

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

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Ketoconazole, CAS 65277-42-1

Pack Size	Availability	Price/USD
50 mg	In stock	$ 33.00
100 mg	In stock	$ 46.00
200 mg	In stock	$ 57.00
500 mg	In stock	$ 72.00
1 g	In stock	$ 97.00
5 g	In stock	$ 367.00
1 mL * 10 mM (in DMSO)	In stock	$ 51.00

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Purity: 99.62%

Purity: 99.61%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.
Targets&IC50	Cyclosporine oxidase:0.19 mM, Testosterone 6β-hydroxylase:0.22 mM
In vitro	Intraperitoneal administration of Ketoconazole (25 mg/kg) in rats significantly reduced plasma corticosterone levels and decreased self-administration of low doses of cocaine. Rats treated with Ketoconazole exhibited enhanced bioavailability of digoxin, increasing from 0.68 to 0.84, with the mean absorption time decreasing from 1.1 h to 0.3 h. Moreover, the oral area under the curve (AUC) for digoxin increased from 63 mg·h/L to 411 mg·h/L, while the intravenous AUC also rose from 93 mg·h/L to 486 mg·h/L.
In vivo	In HT29-S-B6 colorectal cancer cells, Ketoconazole decreased cell proliferation and [3H]thymidine uptake in a dose-dependent manner, with an IC50 of 2.5 mM. Ketoconazole also inhibited [3H]thymidine uptake in both Evsa-T and MDA-MB-231 cell lines, with respective IC50 values of 2 μM and 13 μM. Within 24 hours, Ketoconazole induced a dose-dependent reduction in the S-phase cell population (from 17% to 3%) and a corresponding increase in the Go-G1 phase cell percentage (from 64% to 80%) in HT29-S-B6 cells. By competitively binding with [3H]Dexamethasone, Ketoconazole inhibited fibroblast glucocorticoid receptors, with an IC50 of 0.3 mM. Several Aspergillus species were sensitive to Ketoconazole, with a minimum inhibitory concentration of 0.03 μg/mL.
Kinase Assay	Whole Cell [3H]R1881 Binding Assay: Fibroblasts are grown to confluence in five or six 150 cm2 tissue culture flasks for routine assay. This usually requires 4-6 weeks from the time of the initial seeding of the cell line. All studies are performed between passages 3-20. Two days before assay, the medium is changed to one lacking fetal calf serum. This is repeated again 24 hours before assay. Competition assays are performed with 0.5-1.0 nM [3H]R1881 and increasing amounts of the nonradioactive compounds. Binding to low affinity sites is determined in the presence of 5 × 10-7 M R1881 and is subtracted from whole cell binding of [3H]R 1881 obtained in the absence of any inhibitor to assess binding to 5 high affinity site
Cell Research	HT29-S-B6 cells (5×105) are plated in 35-mm Petri dishes. The next day, the medium is changed and effectors are added in a small volume (10-20 μL). The incubation medium is renewed every day during the experiments. The same triplicate dishes are used for cell counts, [3H]thymidine incorporation, and flow cytometry. [3H]Thymidine (0.5 μCi) is allowed to incorporate for 24 hours; at the end of incubation, cells are rinsed with 1 mL of medium, detached with 1 mL of trypsin-EDTA, and diluted (1:3) with the culture medium. An aliquot (0.5-1 mL) is used for cell count with a Coulter Counter.(Only for Reference)

Synonyms	R-41400, Xolegel, (±)-Ketoconazol, Extina
Molecular Weight	531.43
Formula	C26H28Cl2N4O4
CAS No.	65277-42-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.31 mg/mL (10 mM), Sonification is recommended

References and Literature

1. Oliver WR Jr, et al. Proc Natl Acad Sci U S A, 2001, 98(9), 5306-5311. 2. Eil C, et al. Horm Metab Res, 1992, 24(8), 367-370. 3. Forgue-Lafitte ME, et al. Cancer Res, 1992, 52(24), 6827-6831. 4. Gupta AK, et al. Br J Dermatol, 2000, 142(4), 758-765. 5. Goeders NE, et al. Drug Alcohol Depend, 1998, 53(1), 67-77. 6. Xu J, Liu R, Sun F, et al. Eucalyptal D Enhances the Antifungal Effect of Fluconazole on Fluconazole-Resistant Candida albicans by Competitively Inhibiting Efflux Pump[J]. Frontiers in Cellular and Infection Microbiology. 2019, 9.

Citations

1. Yu H, Song M, Hu K, et al. Influence of Bisphenol Compounds at Nanomolar Concentrations on Chromosome Damage Induced by Metabolically Activated Carcinogens in HepG2 Cells. Environmental Science & Technology. 2021 2. Yu H, Chen Z, Hu K, et al. Potent Clastogenicity of Bisphenol Compounds in Mammalian Cells—Human CYP1A1 Being a Major Activating Enzyme. Environmental Science & Technology. 2020, 54(23): 15267-15276. 3. Song M, Wang Y, Chen Z, et al. Human CYP enzyme-activated genotoxicity of 2, 2′, 4, 4′-tetrabromobiphenyl ether in mammalian cells. Chemosphere. 2021: 132784. 4. Ren L, Li W, Zheng X, et al. Benzimidazoles induce concurrent apoptosis and pyroptosis of human glioblastoma cells via arresting cell cycle. Acta Pharmacologica Sinica. 2021: 1-15. 5. Xu J, Liu R, Sun F, et al. Eucalyptal D Enhances the Antifungal Effect of Fluconazole on Fluconazole-Resistant Candida albicans by Competitively Inhibiting Efflux Pump. Frontiers in Cellular and Infection Microbiology. 2019, 9 6. Zhou L, Tian M, Zhang B, et al.Lysosome targeting fluorescent probe for NAAA imaging and its applications in the drug development for anti-inflammatory.International Journal of Biological Macromolecules.2024: 130307.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library GPCR Compound Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Kinase Inhibitor Library Anti-Cancer Drug Library FDA-Approved Kinase Inhibitor Library

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ketoconazole 65277-42-1 GPCR/G Protein Immunology/Inflammation MAPK Metabolism Microbiology/Virology NADPH-oxidase P450 Hydroxylase Antifungal Ras Inhibitor inhibit Fungal Cytochrome P450 R 41400 Ketoconazol R-41400 CYPs Xolegel R41400 (±)-Ketoconazol Extina inhibitor

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