MW 705.64 g/mol, Purity >99%. Cytochrome p450 CYP3A4 inhibitor (IC50 = 16-26 nM for midazolam hydroxylation). Higher affinity for fungal enzymes over mammalian cytochrome p450. Limited ability to cross the blood-brain barrier. Antifungal activity.
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- Drug metabolism and disposition: the biological fate of chemicals 40:426-352011Stereospecific metabolism of itraconazole by CYP3A4: dioxolane ring scission of azole antifungals.Applications:Unspecified applicationReactive species:Unspecified reactive speciesChi-Chi Peng,Wei Shi,Justin D Lutz,Kent L Kunze,Jun O Liu,Wendel L Nelson,Nina IsoherranenPubMed 22106171
- Drug metabolism and disposition: the biological fate of chemicals 31:319-252003Effect of efflux inhibition on brain uptake of itraconazole in mice infected with Cryptococcus neoformans.Applications:Unspecified applicationReactive species:Unspecified reactive speciesFrédéric Imbert,Méryam Jardin,Christine Fernandez,Jean Charles Gantier,Françoise Dromer,Gabriel Baron,France Mentre,Ludy Van Beijsterveldt,Eric Singlas,François GimenezPubMed 12584159
- Expert opinion on pharmacotherapy 1:287-3042001Itraconazole.Applications:Unspecified applicationReactive species:Unspecified reactive speciesG E Piérard,J E Arrese,C Piérard-FranchimontPubMed 11249550
Key facts
- CAS number
84625-61-6
- Purity
> 99%
- Form
Solid
- Molecular weight
705.64 g/mol
- Molecular formula
C35H38Cl2N8O4
- Nature
Synthetic
Recommended products
MW 705.64 g/mol, Purity >99%. Cytochrome p450 CYP3A4 inhibitor (IC50 = 16-26 nM for midazolam hydroxylation). Higher affinity for fungal enzymes over mammalian cytochrome p450. Limited ability to cross the blood-brain barrier. Antifungal activity.
Key facts
- CAS number
84625-61-6
- Purity
> 99%
- Form
Solid
- Molecular weight
705.64 g/mol
- Molecular formula
C35H38Cl2N8O4
- Nature
Synthetic
- Solubility
Soluble in DMSO to 50 mM. Soluble in ethanol to 10 mM (with warming).
- Biological description
Cytochrome p450 CYP3A4 inhibitor (IC50 = 16-26 nM for midazolam hydroxylation). Higher affinity for fungal enzymes over mammalian cytochrome p450. Limited ability to cross the blood-brain barrier. Antifungal activity.
- IUPAC name
4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one
Storage
- Shipped at conditions
Ambient - Can Ship with Ice
- Appropriate long-term storage conditions
-20°C
- Storage information
It is important to note that this product is reported to be light sensitive, Store in the dark, Store under desiccating conditions
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2 product images
Chemical Structure - Itraconazole, Cytochrome p450 inhibitor (ab120816)
2D chemical structure image of ab120816, Itraconazole, Cytochrome p450 inhibitor
Functional Studies - Itraconazole, Cytochrome p450 inhibitor (ab120816)
HepG2 cells were incubated at 37°C for 24h with vehicle control (0 μM) and different concentrations of itraconazole (ab120816). Increased expression of cytochrome P450 1A1 (ab3568) in HepG2 cells correlates with an increase in nifuroxazide concentration, as described in literature.
Whole cell lysates were prepared with RIPA buffer (containing protease inhibitors and sodium orthovanadate), 10 μg of each were loaded on the gel and the WB was run under reducing conditions. After transfer the membrane was blocked for an hour using 3% milk before being incubated with ab3568 at 1/500 dilution and Anti-beta Actin antibody ab8227 at 1 μg/ml overnight at 4°C. Antibody binding was detected using an anti-rabbit antibody conjugated to HRP (Goat Anti-Rabbit IgG H&L (HRP) ab97051) at 1/10000 dilution and visualised using ECL development solution.
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