Fluconazole-d₄  (Synonyms: UK-49858-d₄)

Fluconazole-d₄ is the deuterium labeled Fluconazole. Fluconazole (UK-49858) is a triazole antifungal agent with excellent activities against a broad range of fungi, especially against Candida albicans. Fluconazole inhibits C. albicans and Candida kefyr with IC99s range from 0.20 μg/mL to 0.39 μg/mL[1].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

310.30

C₁₃H₈D₄F₂N₆O

1124197-58-5

Solid

White to off-white

FC1=CC(F)=C(C=C1)C(O)(C([2H])(N2C=NC=N2)[2H])C([2H])(N3C=NC=N3)[2H]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. H Yamaguchi, et al. [In vitro activity of fluconazole, a novel bistriazole antifungal agent]. Jpn J Antibiot. 1989 Jan;42(1):1-16.  [Content Brief]

  [3]. M A Pfaller, et al. Interpretive breakpoints for fluconazole and Candida revisited: a blueprint for the future of antifungal susceptibility testing. Clin Microbiol Rev. 2006 Apr;19(2):435-47.  [Content Brief]

  [4]. P G Sohnle, et al. Effect of fluconazole on viability of Candida albicans over extended periods of time. Antimicrob Agents Chemother. 1996 Nov;40(11):2622-5.  [Content Brief]

  [5]. A Louie, et al. Pharmacodynamics of fluconazole in a murine model of systemic candidiasis. Antimicrob Agents Chemother. 1998 May;42(5):1105-9.  [Content Brief]