| Name | Itraconazole |
| Description | Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis. |
| In vitro | Like other Hedgehog (Hh) pathway antagonists, Itraconazole can inhibit the activity of the Hh pathway and the growth of medulloblastoma in a murine syngeneic transplant model. |
| In vivo | Itraconazole exhibits affinity for mammalian cytochrome P-450 enzymes and fungal P-450-dependent enzymes, thereby possessing potential for clinically significant interactions with azoles (e.g., simvastatin, terfenadine, rifampin, oral contraceptives, H2 receptor antagonists, warfarin, cyclosporine). Metabolized into hydroxy-itraconazole (OH-ITZ) and two novel metabolites, keto-itraconazole (keto-ITZ) and N-desalkyl itraconazole (ND-ITZ), its metabolites are inhibitors of CYP3A4 as potent, or more so, than itraconazole itself. Itraconazole acts on the hedgehog (Hh) signaling pathway component Smoothened with a mechanism distinct from cyclopamine and other known SMO antagonists, preventing SMO accumulation stimulated by Hh activation. It inhibits 60 clinical isolates of Aspergillus with MICs at 0.25 mg/mL, primarily by damaging ergosterol synthesis, leading to defective fungal cell membranes with altered permeability and function. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 7.06 mg/mL (10 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.71 mg/mL (1.01 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
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| Keywords | Inhibitor | inhibit | Fungal | R-51211 | CYP-450 | Antibiotic | Autophagy | lanosterol | anticancer | Triazole | Hedgehog | ergosterol | Cytochrome P450 | antiangiogenic | antifungal | CYPs | Itraconazole | 14α-demethylase | R 51211 |
| Inhibitors Related | Neomycin sulfate | Ampicillin sodium | Kanamycin sulfate | Sulfamethoxazole sodium | Hydroxychloroquine | Guanidine hydrochloride | Doxycycline | Paeonol | Naringin |
| Related Compound Libraries | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Anti-Fungal Compound Library | Miao medicine Compound Library | Inhibitor Library | Cosmetic Ingredient Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
