Synonym: Oriconazole, R51211, Sporanox
CAS Number: 84625-61-6
Empirical Formula (Hill Notation): C35H38Cl2N8O4
Molecular Weight: 705.63
MDL Number: MFCD00870168
Application
Itraconazole is a triazole antifungal agent. It is used to inhibit cytochrome P-450-dependent enzymes and ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis, and aspergillosis. It′s different formulations are used to study Candida strains in murine invasive infections1. It has been used to study proliferative changes of the forestomach mucosa in alloxan-induced diabetic rats2.
Biochem/physiol Actions
Itraconazole inhibits cytochrome P-450-dependent enzymes which results in the inhibition of ergosterol synthesis. It does so by interacting with 14-α demethylase, which is a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. Ergosterol is a crucial compenent of fungal cell membranes. Therefore, it′s inhibition results in increased cellular permeability causing leakage of cellular contents. Itraconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and phospholipid biosynthesis.
Assay: ≥98% (TLC)
Solubility: Chloroform: soluble50 mg/mL, clear, colorless
Storage Temp.: 2-8°C