Fosfluconazole

SKU: orb1301884

Description

Fosfluconazole is a water-soluble phosphate prodrug of the antifungal agent fluconazole. It is designed for research applications, including in vitro antifungal susceptibility testing and in vivo models of systemic fungal infections.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 194798-83-9
• MW: 386.25
• Purity: 99.12% (May vary between batches)
• Formula: C₁₃H₁₃F₂N₆O₄P
• SMILES: C(CN1C=NC=N1)(CN2C=NC=N2)(OP(=O)(O)O)C3=C(F)C=C(F)C=C3
• Target: Antifungal
• Solubility: DMSO:6 mg/mL (15.53 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.59 mM)

Bioactivity

• In Vivo:
  Fosfluconazole was administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ was detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration was lower than that after the intravenous (i.v.) F-FLCZ administration .
• In Vitro:
  In Caco-2 monolayer, 10 μM Fosfluconazole is dosed either in the apical or basal compartment in Transwell plates. Both prodrugs are efficiently cleaved in the apical compartment after a 2 h incubation. The rate of ALP-mediated conversion was prodrug concentration-dependent with Michaelis-Menten constants of 351 μM for fosfluconazole, determined in Caco-2 cells .
• Animal Research:
  Twelve-week-old male Wistar rats (200–300 g) were used. They were housed in a temperature-controlled room and were given food and water ad libitum. All rats were anesthetized by an i.p. administration of pentobarbital (50 mg/kg body weight). A catheter was placed in the peritoneal cavity and used as an inflow drain for the dialyzing fluid. sampling. In rats receiving i.v. administration, a catheter was inserted into the left jugular vein for drug administration, and another into the right femoral artery for blood sampling. Blood samples after the i.p. administration were obtained from the heart. The rats were then allowed to recover from the anesthesia and surgery for at least 24 hr. After the 40-mL dialyzing fluid was administered intraperitoneally, FLCZ 16 mg/kg body weight) and F-FLCZ (16 mg FLCZ eq/kg body weight) were administered intravenously. The volume of the drug solution administered intravenously was 8 mL/kg. FLCZ (16 mg/kg body weight) and F-FLCZ (16 mg FLCZ eq/kg body weight) dissolved in the 40 mL of dialyzing fluid were administered intraperitoneally. The dialyzing fluid FLCZ concentration was 100 mg/L. F-FLCZ (16 mg FLCZ eq/kg body weight) was administered to ARF rats intravenously and intraperitoneally. Blood (0.5 mL) and dialyzing ‰uid (1.5 mL) samples were collected at appropriate time intervals .

Storage & Handling

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

Alternative Names

inhibit, Fosfluconazole, Fungal, Inhibitor, Antifungal

Compound Identifiers

PubChem CID

214356