Fluconazole (UK 49858)

For research use only.

Licensed by Pfizer Catalog No.S1331

11 publications

Fluconazole (UK 49858) Chemical Structure

CAS No. 86386-73-4

Fluconazole (UK 49858) 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.

Selleck's Fluconazole (UK 49858) has been cited by 11 publications

Purity & Quality Control

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Biological Activity

Description Fluconazole (UK 49858) 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

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 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]

Protocol

Solubility (25°C)

In vitro DMSO 61 mg/mL (199.17 mM)
Water Insoluble
Ethanol ''61 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
12mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 306.27
Formula

C13H12F2N6O

CAS No. 86386-73-4
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=C(C=C1F)F)C(CN2C=NC=N2)(CN3C=NC=N3)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04933682 Recruiting Drug: ALXN2050|Drug: Fluconazole|Drug: Rifampin Healthy Alexion Pharmaceuticals June 2021 Phase 1
NCT04871724 Completed Drug: EDP-938|Drug: Fluconazole RSV Infection Enanta Pharmaceuticals March 12 2021 Phase 1
NCT04621253 Completed Drug: Novalgin Drug-drug Interaction University Hospital Basel Switzerland April 29 2020 Phase 1
NCT04122560 Completed Drug: Fluconazole 200mg tab|Drug: Fluconazole 2 MG/ML Fluconazole|Candidiasis|Invasive Fungal Infections|Obesity Radboud University|St. Antonius Hospital November 30 2019 Phase 4
NCT04038008 Unknown status Drug: Fluconazole|Drug: Diflucan® Bioequivalence Pharmtechnology LLC|Altasciences Company Inc. July 2019 Phase 1

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID