| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
The active metabolite of itraconazole (ITZ) is hydroxyitraconazole (itraconazole metabolite hydroxyitraconazole; R-63373). Despite reports of in vitro antifungal effectiveness, hydroxyitraconazole's human pharmacokinetic research has not been as extensive as that of ITZ. Because they include a triazole ring, ITZ and hydroxyitraconazole block CYP3A. Reusable medications have a half-life that is 26–60% longer than that of single-use medications [1].
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| ln Vivo |
The method by which hydroxyitraconazole has been absorbed is most likely what causes the concentration of hydroxyitraconazole, which is only marginally influenced by the dose of ITZ. ITZ and hydroxyitraconazole pharmacokinetics may be affected by serum albumin and GFR. It's crucial to take into account both the intravenous concentration of ITZ and the concentration of hydroxyitraconazole when talking about antifungal activity. However, the pharmacokinetics of hydroxyitraconazole are identical to those of ITZ in immunocompromised individuals receiving the intravenous solution of the drug. Given the strong relationship between the intravenous concentrations of ITZ and hydroxyitraconazole, the clinically measured Marathon concentration ought to be enough [1].
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Hydroxy-iteraconazole is a known human metabolite of itraconazole. |
| References | |
| Additional Infomation |
See also: Hydroxyitraconazole (annotation moved to).
|
| Molecular Formula |
C35H38CL2N8O5
|
|---|---|
| Molecular Weight |
721.64
|
| Exact Mass |
720.234
|
| CAS # |
112559-91-8
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| Related CAS # |
Hydroxy Itraconazole-d8;(2R,4S)-Hydroxy Itraconazole-d5;1217524-77-0;Itraconazole;84625-61-6;(2R,4S)-Hydroxy Itraconazole-d8;1217516-26-1
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| PubChem CID |
108222
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| Appearance |
White to off-white solid powder
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| Density |
1.44g/cm3
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| Boiling Point |
884.7ºC at 760mmHg
|
| Melting Point |
76-78ºC
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| Flash Point |
488.8ºC
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| Vapour Pressure |
0mmHg at 25°C
|
| Index of Refraction |
1.687
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| LogP |
4.967
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
50
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ISJVOEOJQLKSJU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C35H38Cl2N8O5/c1-24(25(2)46)45-34(47)44(23-40-45)29-6-4-27(5-7-29)41-13-15-42(16-14-41)28-8-10-30(11-9-28)48-18-31-19-49-35(50-31,20-43-22-38-21-39-43)32-12-3-26(36)17-33(32)37/h3-12,17,21-25,31,46H,13-16,18-20H2,1-2H3
|
| Chemical Name |
4-[4-[4-[4-[[2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-(3-hydroxybutan-2-yl)-1,2,4-triazol-3-one
|
| Synonyms |
R-63373; R 63373; Hydroxyitraconazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~115.47 mM)
H2O : ~1 mg/mL (~1.39 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3857 mL | 6.9287 mL | 13.8573 mL | |
| 5 mM | 0.2771 mL | 1.3857 mL | 2.7715 mL | |
| 10 mM | 0.1386 mL | 0.6929 mL | 1.3857 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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