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

Cat. No.: HY-12772 Purity: 99.74%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 112559-91-8

Size	Price	Stock	Quantity
1 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Hydroxy Itraconazole:

Hydroxy Itraconazole-d₈ In-stock
(2R,4S)-Hydroxy Itraconazole-d₅ In-stock
Itraconazole In-stock
(2R,4S)-Hydroxy Itraconazole-d₈ Get quote

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Biological Activity
Purity & Documentation
References
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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].

MedChemExpress (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].

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

Molecular Weight

721.63

Formula

C₃₅H₃₈Cl₂N₈O₅

CAS No.

112559-91-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(N=C1)C(C)C(O)C)N1C(C=C2)=CC=C2N(CC3)CCN3C(C=C4)=CC=C4OC[C@H](CO5)O[C@@]5(C6=C(C=C(C=C6)Cl)Cl)CN7C=NC=N7

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 : 83.33 mg/mL (115.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (250 KB) HNMR (324 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Mino Y, et al. Hydroxy-itraconazole pharmacokinetics is similar to that of itraconazole in immunocompromised patients receiving oral solution of itraconazole. Clin Chim Acta. 2013 Jan 16;415:128-32. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3858 mL	6.9288 mL	13.8575 mL	34.6438 mL
	5 mM	0.2772 mL	1.3858 mL	2.7715 mL	6.9288 mL
	10 mM	0.1386 mL	0.6929 mL	1.3858 mL	3.4644 mL
	15 mM	0.0924 mL	0.4619 mL	0.9238 mL	2.3096 mL
	20 mM	0.0693 mL	0.3464 mL	0.6929 mL	1.7322 mL
	25 mM	0.0554 mL	0.2772 mL	0.5543 mL	1.3858 mL
	30 mM	0.0462 mL	0.2310 mL	0.4619 mL	1.1548 mL
	40 mM	0.0346 mL	0.1732 mL	0.3464 mL	0.8661 mL
	50 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6929 mL
	60 mM	0.0231 mL	0.1155 mL	0.2310 mL	0.5774 mL
	80 mM	0.0173 mL	0.0866 mL	0.1732 mL	0.4330 mL
	100 mM	0.0139 mL	0.0693 mL	0.1386 mL	0.3464 mL

Hydroxy Itraconazole Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hydroxy Itraconazole112559-91-8Itraconazole metabolite Hydroxy Itraconazole R-63373R63373R 63373R-63373FungalDrug MetaboliteInhibitorinhibitorinhibit

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