| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 8 mg/mL (11.34 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.71 mg/mL (1.01 mM), Suspension.
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| Keywords | Triazole | Smoothened | R-51211 | R 51211 | lanosterol | Itraconazole | Inhibitor | inhibit | Hedgehog | Fungal | ergosterol | Cytochrome P450 | CYPs | CYP-450 | CYP3A4 | Autophagy | antifungal | anticancer | Antibiotic | antiangiogenic | 14α-demethylase |
| Inhibitors Related | Neomycin sulfate | Calcium Propionate | Aceglutamide | Hemin | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Benzyl propionate | Sulfamethoxazole sodium | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate |
| Related Compound Libraries | Anti-Fungal Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bitter Compound library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Cosmetic Ingredient Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
