Fluconazole

SKU: orb1223822

Description

Triazole antifungal agent that is used to treat oropharyngeal candidiasis and cryptococcal meningitis in AIDS. (In Vitro):Fluconazole inhibits 4 species ofAspergillus fumigatus with the IC50s of 23.9-43.5 μg/mL. Fluconazole (0.20 μg/mL) inhibits significantly the mycelial-phase growth and germ tube elongation of C. albicans in a medium supplemented with serum.Fluconazole is a triazole antifungal agent that has been available for the treatment of infections due to Candida, Cryptococcus. The MIC90 is highest for C. krusei (MIC ≥ 64 μg/mL) and C. glabrata (MIC, 32 μg/mL) and is ≤2 μg/mL for C. albicans (0.5 μg/mL), C. parapsilosis (2 μg/mL), C. tropicalis (2 μg/mL), C. lusitaniae (2 μg/mL), and C. kefyr (0.5 μg/mL).Fluconazole (0.1-50.0 μg/mL) damages the fungal cells and reduces their viability.(In Vivo):Fluconazole ( 0, 0.5, 1, 2.5, 5, 7.5, and 10 mg/kg; administered intraperitoneally (i.p.) as a single dose) results in a 50% reduction in fungal densities (ED50) of 4.87 mg/kg in a murine model of systemic candidiasis. Fluconazole exhibits terminal elimination half-life of 2.4 h) following i.p.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 86386-73-4
• MW: 306.27
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₂F₂N₆O
• SMILES: OC(CN1N=CN=C1)(C2=CC=C(F)C=C2F)CN3N=CN=C3
• Target: Antifection
• Solubility: Ethanol: 61 mg/mL (199.17 mM); DMSO: 61 mg/mL (199.17 mM)

Bioactivity

• In Vivo:
  Animal model: Female NYLAR mice (weight, 18 to 20 g; infected intravenously with C. albicans blastoconidia). Dosage: 5, 10, 15 and 20 mg/kg (Pharmacokinetic Analysis). Administration: Given i.p. as a single dose. Result: T1/2 = 2.4 h.
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• In Vitro:
  Cell Viability Assay Cell line: C. albicans yeast cells (strain ATCC 26310 and strain TW) Concentration: 0.1, 0.5, 5.0, 50.0 μg/mL Incubation time: 24 hours. Result: The MICs against both strains were 0.5 μg/mL.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

UK 49858

Quick Database Links

Gene Symbol

Antifection