製品名Itraconazole, Cytochrome p450 inhibitor
製品の詳細Cytochrome p450 inhibitor
- R 51211
生理活性の詳細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.
保存方法Store at -20°C. It is important to note that this product is reported to be light sensitive. Store In the Dark. Store under desiccating conditions.
溶解性Soluble in DMSO to 50 mM and in ethanol to 10 mM (with warming)
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Our Abpromise guarantee covers the use of ab120816 in the following tested applications.
The application notes include recommended starting dilutions; optimal dilutions/concentrations should be determined by the end user.
|Functional Studies||Use at an assay dependent concentration.|
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 ab8227 at 1 µg/ml overnight at 4°C. Antibody binding was detected using an anti-rabbit antibody conjugated to HRP (ab97051) at 1/10000 dilution and visualised using ECL development solution.
This product has been referenced in:
- Peng CC et al. Stereospecific metabolism of itraconazole by CYP3A4: dioxolane ring scission of azole antifungals. Drug Metab Dispos 40:426-35 (2012). Read more (PubMed: 22106171) »
- Imbert F et al. Effect of efflux inhibition on brain uptake of itraconazole in mice infected with Cryptococcus neoformans. Drug Metab Dispos 31:319-25 (2003). Read more (PubMed: 12584159) »
- Piérard GE et al. Itraconazole. Expert Opin Pharmacother 1:287-304 (2000). Read more (PubMed: 11249550) »