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Hydroxy Itraconazole

Cat. No. M1587
Hydroxy Itraconazole Structure
Synonym:

Hydroxy Itraconazole; R-63373

Size Price Availability
1mg USD 300  USD300 Out of stock
5mg USD 900  USD900 Out of stock
10mg USD 1600  USD1600 Out of stock
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Quality Control & Documentation
Biological Activity

Itraconazole metabolite Hydroxy Itraconazole is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

Chemical Information
Molecular Weight 721.63
Formula C35H38Cl2N8O5
CAS Number 112559-91-8
Form Solid
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nathan P Wiederhold, et al. Variability of Hydroxy-Itraconazole in Relation to Itraconazole Bloodstream Concentrations

[2] Nicole Jenkins, et al. Simultaneous determination of voriconazole, posaconazole, itraconazole and hydroxy-itraconazole in human plasma using LCMS/MS

[3] K De Beule, et al. Pharmacology of itraconazole

[4] J W Hlsewede, et al. Determination of itraconazole and hydroxy-itraconazole in sera using high-performance-liquid-chromatography and a bioassay

[5] R Negroni, et al. Itraconazole: pharmacokinetics and indications

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