Fluconazole

Catalog No.S1331 Batch:S133101

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Technical Data

Formula

C13H12F2N6O

Molecular Weight 306.27 CAS No. 86386-73-4
Solubility (25°C)* In vitro DMSO 61 mg/mL (199.17 mM)
Ethanol 61 mg/mL (199.17 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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 (from reference)

Selleck's Fluconazole has been cited by 24 publications

In vitro interactions of proton pump inhibitors and azoles against pathogenic fungi [ Front Cell Infect Microbiol, 2024, 14:1296151] PubMed: 38304196
Interactions between antifungals and everolimus against Cryptococcus neoformans [ Front Cell Infect Microbiol, 2023, 13:1131641] PubMed: 37026056
BAF complex-mediated chromatin relaxation is required for establishment of X chromosome inactivation [ Nat Commun, 2022, 13(1):1658] PubMed: 35351876
Maternal SMCHD1 regulates Hox gene expression and patterning in the mouse embryo [ Nat Commun, 2022, 13(1):4295] PubMed: 35879318
Maternal SMCHD1 regulates Hox gene expression and patterning in the mouse embryo [ Nat Commun, 2022, 13(1):4295] PubMed: 35879318
Synergistic effect of pyrvinium pamoate and posaconazole against Cryptococcus neoformans in vitro and in vivo [ Front Cell Infect Microbiol, 2022, 12:1074903] PubMed: 36569209
Terconazole, an Azole Antifungal Drug, Increases Cytotoxicity in Antimitotic Drug-Treated Resistant Cancer Cells with Substrate-Specific P-gp Inhibitory Activity [ Int J Mol Sci, 2022, 23(22)13809] PubMed: 36430288
A Preliminary in vitro and in vivo Evaluation of the Effect and Action Mechanism of 17-AAG Combined With Azoles Against Azole-Resistant Candida spp [ Front Microbiol, 2022, 13:825745] PubMed: 35875545
A method for stabilising the XX karyotype in female mESC cultures [ Development, 2022, 149(22)dev200845] PubMed: 36355065
A method for stabilising the XX karyotype in female mESC cultures [ Development, 2022, 149(22)dev200845] PubMed: 36355065

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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