Home Metabolism P450 (e.g. CYP17) inhibitor - Fungal inhibitor Fluconazole For research use only.

Fluconazole

Synonyms: UK 49858

Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.

Fluconazole Chemical Structure

Fluconazole Chemical Structure

CAS No. 86386-73-4

Purity & Quality Control

Fluconazole Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Biological Activity

Description Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.
Targets
lanosterol 14 alpha-demethylase [1]
In vitro
In vitro

Fluconazole in combination with amphotericin B (AmB) has a synergistic effect on C. albicans planktonic cells but does not alter AmB activity against biofilms. Fluconazole and caspofungin have an antagonistic effect against biofilms but not with planktonic cells. Fluconazole-mediated membrane perturbation (due to inhibition of ergosterol biosynthesis) increases calcineurin inhibitor intracellular concentrations. Fluconazole treatment significantly reduces levels of ergosterol within the cell in C. albicans planktonic cells, leading to cell membrane perturbation. [1] Fluconazole activity is less sensitive to acidic medium than is that of ketoconazole. Fluconazole is approximately 16-fold less active than ketoconazole against 35 representative isolates of C. albicans at physiologic pH. [2] Fluvastatin, a cholesterol-lowering drug, exhibits minimal activity (MICs of 64 to >128 mg/mL) against Candida species and Cryptococcus neoformans. Fluconazole combined with itraconazole exhibits potent activities against C. albicans, C. tropicalis, C. parapsilosis, and C. neoformans, including flucon- azole-resistant strains of C. albicans and C. tropicalis. [3]
In Vivo
In vivo

Fluconazole is very effective in prolonging survival of rats infected with a representative candidal strain. [3] Fluconazole has a dramatic effect on the fungicidal activity of flucytosine in murine cryptococcal meningitis. Fluconazole combined with flucytosine and amphotericin B have significantly improved activity against cryptococcal meningitis compared with the activity of each drug used alone. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05130723 Recruiting
Invasive Fungal Infections
Radboud University Medical Center
 October 18 2022 --
NCT04933682 Completed
Healthy
Alexion Pharmaceuticals Inc.
 June 23 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 306.27 Formula

C13H12F2N6O
CAS No. 86386-73-4 SDF Download Fluconazole SDF
Smiles C1=CC(=C(C=C1F)F)C(CN2C=NC=N2)(CN3C=NC=N3)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 61 mg/mL ( (199.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 61 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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