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Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
50 mg | $34 | In Stock | |
100 mg | $48 | In Stock | |
200 mg | $77 | In Stock | |
500 mg | $178 | In Stock |
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. |
Alias | R51211 |
Molecular Weight | 705.63 |
Formula | C35H38Cl2N8O4 |
Cas No. | 84625-61-6 |
Smiles | C([C@]1(O[C@@H](COC2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)N5C(=O)N(C(CC)C)N=C5)CO1)C6=C(Cl)C=C(Cl)C=C6)N7C=NC=N7 |
Relative Density. | 1.4 g/cm3 |
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), In vivo: 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. | |||||||||||||||
Solution Preparation Table | ||||||||||||||||
DMSO
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