1. Anti-infection
    Metabolic Enzyme/Protease
  2. Fungal
    Drug Metabolite
  3. Hydroxy Itraconazole

Hydroxy Itraconazole (Synonyms: Itraconazole metabolite Hydroxy Itraconazole; R-63373)

Cat. No.: HY-12772 Purity: 99.60%
Handling Instructions

Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

For research use only. We do not sell to patients.

Hydroxy Itraconazole Chemical Structure

Hydroxy Itraconazole Chemical Structure

CAS No. : 112559-91-8

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1 mg USD 252 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
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Description

Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ), which is a triazole antifungal agent.

IC50 & Target

Antifungal[1]

In Vitro

Hydroxy Itraconazole (Itraconazole metabolite Hydroxy Itraconazole; R-63373) is an active metabolite of Itraconazole (ITZ). Although Hydroxy Itraconazole is also reported to have antifungal activity in vitro, its pharmacokinetics in humans has been studied less than that of ITZ. ITZ and Hydroxy Itraconazole have a triazole ring and inhibit CYP3A. Their half-lives can be extended by 26-60% with repeated administration compared to single administration[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The plasma concentration of Hydroxy Itraconazole is weakly dependent on the dose of ITZ, most likely because the process that forms Hydroxy Itraconazole is saturated. Serum albumin and GFR may alter the pharmacokinetics of ITZ and Hydroxy Itraconazole. Antifungal activity should be discussed while taking into account not only the plasma concentration of ITZ but also that of Hydroxy Itraconazole. However, the pharmacokinetics of Hydroxy Itraconazole is similar to that of ITZ in immunocompromised patients taking an oral solution of ITZ. Since the plasma concentrations of ITZ and Hydroxy Itraconazole are closely correlated, determining the plasma concentration of either should be sufficient from a clinical point of view[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

721.63

Formula

C₃₅H₃₈Cl₂N₈O₅

CAS No.
SMILES

O=C1N(C(C)C(O)C)N=CN1C2=CC=C(N3CCN(C4=CC=C(OCC5OC(CN6N=CN=C6)(C7=CC=C(Cl)C=C7Cl)OC5)C=C4)CC3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (138.58 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3858 mL 6.9288 mL 13.8575 mL
5 mM 0.2772 mL 1.3858 mL 2.7715 mL
10 mM 0.1386 mL 0.6929 mL 1.3858 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (3.46 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (3.46 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.60%

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Keywords:

Hydroxy ItraconazoleItraconazole metabolite Hydroxy Itraconazole R-63373R63373R 63373R-63373FungalDrug MetaboliteInhibitorinhibitorinhibit

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Product Name:
Hydroxy Itraconazole
Cat. No.:
HY-12772
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