product name Fluconazole
Description: Fluconazole is an orally available antifungal medication that inhibits fungal lanosterol 14 alpha-demethylase, it prevents the formation of ergosterol. Fluconazole is used to treat a variety of fungal infections, especially Candida infections of the vagina, mouth, throat, and bloodstream. It is also used to prevent infections in people with weak immune systems, including those with neutropenia due to cancer chemotherapy, transplant patients, and premature babies.
References: Antimicrob Agents Chemother. 2008 Mar;52(3):1127-32; Antimicrob Agents Chemother. 1996 Sep;40(9):2178-82.
306.27
Formula
C13H12F2N6O
CAS No.
86386-73-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 61 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 61 mg/mL (199.2 mM)
Solubility (In vivo)
Synonyms
UK 49858
other peoduct :
| In Vitro |
In vitro activity: 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. 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Fluconazole is very effective in prolonging survival of rats infected with a representative candidal strain. 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. |
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| Formulation & Dosage | |
| References | Cancer Cell. 2010 Apr 13;17(4):388-99; Antimicrob Agents Chemother. 2008 Mar;52(3):1127-32; Antimicrob Agents Chemother. 1996 Sep;40(9):2178-82. |
