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Itraconazole

Itraconazole
Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.
Catalog No. T1011Cas No. 84625-61-6
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Itraconazole

Catalog No. T1011Cas No. 84625-61-6
Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.
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Pack SizePriceAvailabilityQuantity
50 mg$34In Stock
100 mg$48In Stock
200 mg$77In Stock
500 mg$178In Stock
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Product Introduction

Bioactivity
Description
Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.
Targets&IC50
CYP3A4:6.1 nM
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.
AliasR51211
Chemical Properties
Molecular Weight705.63
FormulaC35H38Cl2N8O4
Cas No.84625-61-6
Storage & Solubility Information
StoragePowder: -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.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.4172 mL7.0859 mL14.1717 mL70.8587 mL
5 mM0.2834 mL1.4172 mL2.8343 mL14.1717 mL
10 mM0.1417 mL0.7086 mL1.4172 mL7.0859 mL

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