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    Fluconazole (UK49858)
    Fluconazole (UK49858)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0806
    CAS #: 86386-73-4Purity ≥98%

    Description: Fluconazole (Diflucan, UK-49858; UK 49858; Triflucan, Elazor, Biozolene) is a novel, potent, and orally bioavailable triazole-based antifungal drug that works by inhibiting fungal lanosterol 14 alpha-demethylase-dependent biosynthesis of ergosterol, which is an essential component of fungal cell membrane. 

    References: Antimicrob Agents Chemother. 2008 Mar;52(3):1127-32; Antimicrob Agents Chemother. 1996 Sep;40(9):2178-82.

    Related CAS: 159532-41-9 (Fluconazole mesylate; UK 49858 mesylate); 155347-36-7 (Fluconazole hydrate); 194798-83-9 (Fosfluconazole)

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    Molecular Weight (MW)306.27
    FormulaC13H12F2N6O
    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)
    Other infoChemical Name: 2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-ol
    InChi Key: RFHAOTPXVQNOHP-UHFFFAOYSA-N
    InChi Code: InChI=1S/C13H12F2N6O/c14-10-1-2-11(12(15)3-10)13(22,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9,22H,4-5H2
    SMILES Code: OC(CN1N=CN=C1)(C2=CC=C(F)C=C2F)CN3N=CN=C3
    SynonymsUK 49858; Fluconazole, Diflucan, UK-49858; UK49858; Triflucan, Elazor, Biozolene


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    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.

    In VivoFluconazole 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.
    Animal modelRats
    Formulation & DosageN/A
    ReferencesCancer 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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Fluconazole

    Impact of fluconazole and FK506 alone and in combination as lock therapy against C. albicans biofilm cells in an in vivo catheter model. Antimicrob Agents Chemother. 2008 Mar; 52(3): 1127–1132.

    Fluconazole

    C. albicans biofilms are hypersensitive to the tacrolimus (FK506)-fluconazole combination. Antimicrob Agents Chemother. 2008 Mar; 52(3): 1127–1132.
     


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