Fluconazole Inhibitor CAS No. 86386-73-4

Cat. No.	Name	Size	Price	Add Cart
KI1039	Fluconazole	500 mg	$104
KI1039	Fluconazole	1 g	$164

Chemical Characteristic

Product Name	Fluconazole
Synonyms	UK 49,858
CAS No.	86386-73-4
Molecular Weight	306.27
Formula	C₁₃H₁₂F₂N₆O
Chemical Name	alpha-(2,4-Difluorophenyl)-alpha-(1H-1,2,4-triazol-1-ylmethyl)-1H-1,2,4-triazole-1-ethanol
Smiles	n1(ncnc1)CC(O)(Cn1ncnc1)c1c(cc(cc1)F)F
Chemical Structure

Biological activities

Fluconazole is a new bis-triazole antifungal agent. Fluconazole is used in the treatment of both C. albicans and dermatophyte fungal infections. In vitro, fluconazole inhibits α-OH-triazolam formation and 4-OH-triazolam formation with IC50 of 4.35 and 4.85 µM, respectively.^[1] The activity of fluconazole given orally to mice or rats infected systemically with C. albicans is far superior to that of ketoconazole. Fluconazole is also effective orally in curing experimental candidal vaginitis in mice and trichophytosis in guinea pigs, against which it is approximately 10 times more active than ketoconazole. ^[2] In a 10-day dosage regimen, fluconazole is far more active than ketoconazole against systemic infections with C. albicans in normal and immunosuppressed mice. In normal mice, extension of fluconazole dosing to 30 days results in prolongation of survival to over 90 days, and up to 60% of treated animals had no detectable C. albicans in their kidneys. ^[3]

Protocols

Fluconazole is formulated as suspension in 10% Cremophor EL in 50 mM sodium phosphate buffer, pH 7.0. ^[2]

References

[1] VON MOLTKE LL, et al. Inhibition of Triazolam Hydroxylation by Ketoconazole, Itraconazole, Hydroxyitraconazole and Fluconazole In-vitro. Pharmacy and Pharmacology Communications. 1998, 4(9): 443??45. [2] Richardson K, et al. Activity of UK-49,858, a bis-triazole derivative, against experimental infections with Candida albicans and Trichophyton mentagrophytes. Antimicrob Agents Chemother. 1985, 27(5): 832-835. [3] Troke PF, et al. Efficacy of UK-49,858 (fluconazole) against Candida albicans experimental infections in mice. Antimicrob Agents Chemother. 1985, 28(6): 815-818.

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