Voriconazole
Based on 11 publication(s) in Google Scholar
Voriconazole (UK-109496) is a second-generation, broad-spectrum triazole antifungal agent that inhibits fungal ergosterol biosynthesis. Voriconazole exerts its antifungal activity by inhibition of 14-α-lanosterol demethylation, which is mediated by fungal cytochrome P450 enzymes. Voriconazole can penetrate the blood brain barrier (BBB).
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 137234-62-9
- Formula: C16H14F3N5O
- Molecular Weight:349.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Voriconazole
More- Transl Res. 2022 Sep:247:39-57. [Abstract]
- Front Cell Infect Microbiol. 2020 Jun 26;10:320. [Abstract]
- BMC Microbiol. 2025 Nov 5;25(1):715. [Abstract]
- Microchem J. 2026 Mar 27.
- Microbiol Spectr. 2025 Mar 31:e0318524. [Abstract]
- Drug Metab Dispos. 2025 Nov;53(11):100168. [Abstract]
- Med Mycol. 2018 Jun 1;56(4):452-457. [Abstract]
- Infect Drug Resist. 2022 Dec 15:15:7459-7473. [Abstract]
- J Mycol Med. 2022 Mar;32(1):101227. [Abstract]
- Laryngoscope Investig Otolaryngol. 2022 Oct 28;7(6):1780-1789. [Abstract]
- bioRxiv. 2025 Oct 14:2025.10.13.682145. [Abstract]
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Microbiological Assay
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Microbiological Assay
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Others
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>30 μM
Compound: VOR
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Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay
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[PMID: 34388384] |
| CHO | IC50 |
>40 μM
Compound: 3
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Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay
Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay
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[PMID: 24564525] |
| CHO | IC50 |
414.2 μM
Compound: voriconazole
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Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
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[PMID: 23812503] |
| Hepatocyte | IC50 |
13 μM
Compound: Voriconazole
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Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method
Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method
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[PMID: 24948565] |
| MCF7 | IC50 |
>30 μM
Compound: VOR
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay
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[PMID: 34388384] |
| MRC5 | IC50 |
40 μg/mL
Compound: VOR
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Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
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[PMID: 26867487] |
| MRC5 | IC50 |
40 μg/mL
Compound: Voriconazole
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Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
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[PMID: 26586600] |
| THLE-2 | IC50 |
>30 μM
Compound: VOR
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Cytotoxicity against human THLE-2 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay
Cytotoxicity against human THLE-2 cells assessed as reduction in cell viability measured after 96 hrs by MTT assay
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[PMID: 34388384] |
Voriconazole has great activity against S. apiospermum and C. neoformans with the MICs of 0.5 μg/mL and 0.125-0.25 μg/mL, respectively[1].
Voriconazole inhibits the cytochrome P450 (CYP)-dependent enzyme 14-alpha-sterol demethylase, thereby disrupting the cell membrane and halting fungal growth[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male specific-pathogen-free BALB/cByJ mice[3]
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Dosage:1, 5, 20 mg/kg/day
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Administration:P.o. once daily for 21 days
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Result:Improved survival in a dose-response fashion, with median survival times (MSTs) of 21, 28, and 35 days with doses of 1, 5, and 20 mg/kg, respectively.
Chemical Information
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CAS No. 137234-62-9
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Appearance Solid
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Molecular Weight 349.31
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Formula C16H14F3N5O
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Color White to off-white
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SMILES
O[C@@](CN1N=CN=C1)(C2=CC=C(F)C=C2F)[C@H](C3=NC=NC=C3F)C
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Synonyms
UK-109496
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (11)
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Journal Impact Factor
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Most Recent
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Transl Res
A dual action small molecule enhances azoles and overcomes resistance through co-targeting Pdr5 and Vma1. [Abstract]2022 Sep:247:39-57. PMID: 35452875 -
Front Cell Infect Microbiol
Caenorhabditis elegans- Based Aspergillus fumigatus Infection Model for Evaluating Pathogenicity and Drug Efficacy. [Abstract]2020 Jun 26;10:320. PMID: 32670897
Voriconazole purchased from MedChemExpress. Usage Cited in: Front Cell Infect Microbiol. 2020 Jun 26;10:320. [Abstract]
Kaplan-Meier survival plots of C. elegans infected by KU80Δ in the presence of antifungal drugs. The glp-4(bn2); sek-1(km4) worms were pre-infected with KU80Δ for 8 h then transferred into liquid killing media containing different concentrations of Voriconazole (0-1.5 μg/mL).
Voriconazole purchased from MedChemExpress. Usage Cited in: Front Cell Infect Microbiol. 2020 Jun 26;10:320. [Abstract]
Effect of antifungal treatment on Af293-dsRed infection to glp-4(bn2); sek-1(km4) worms. Images were taken under DIC and TRITC channels from DMSO treatment by 24 h, 1.5 μg/ml AmB treatment by 48 h, 2 μg/ml ItrZ treatment by 72 h and 0.5 μg/ml Voriconazole treatment by 72 h. Scale bar is 200 μm.
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BMC Microbiol
In vitro combination effects and mechanisms of Revaprazan with Triazole antifungal drugs on Aspergillus. [Abstract]2025 Nov 5;25(1):715. PMID: 41194018
Voriconazole purchased from MedChemExpress. Usage Cited in: BMC Microbiol. 2025 Nov 5;25(1):715. [Abstract]
Interaction profile of REV combined with ITR, Voriconazole and POS against Aspergillus spp.
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Microbiol Spectr
Synergistic antifungal activity of minocycline as an effective augmenting agent of fluconazole against drug-resistant Candida tropicalis. [Abstract]2025 Mar 31:e0318524. PMID: 40162832
Voriconazole purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2025 Mar 31:e0318524. [Abstract]
MIC values of antifungal drugs (Voriconazole) against CT27.
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Drug Metab Dispos
Metabolic flux analysis of bile acid biosynthesis acidic pathway in HepG2 cells reveals CYP8B1 inhibition of azole antifungals. [Abstract]2025 Nov;53(11):100168. PMID: 41124962 -
Med Mycol
2018 Jun 1;56(4):452-457. PMID: 29420769 -
Infect Drug Resist
Correlation Between Drug Resistance and Virulence of Candida Isolates from Patients with Candidiasis. [Abstract]2022 Dec 15:15:7459-7473. PMID: 36544991 -
J Mycol Med
In vitro synergistic effect of minocycline combined with antifungals against Cryptococcus neoformans. [Abstract]2022 Mar;32(1):101227. PMID: 34800920 -
Laryngoscope Investig Otolaryngol
Clinical and mycological investigations of post-COVID-19 acute invasive fungal sinusitis. [Abstract]2022 Oct 28;7(6):1780-1789. PMID: 36544940 -
bioRxiv
Cyp7b1-inhibiting azoles as novel enhancers of hematopoietic stem and progenitor cell mobilization. [Abstract]2025 Oct 14:2025.10.13.682145. PMID: 41279189
Voriconazole purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 14:2025.10.13.682145. [Abstract]
Experimental design for HSPC mobilization. Wild-type C57BL/6J or Townes SCD mice were treated with Voriconazole (50 mg/kg/day, iv) or vehicle intravenously daily for four days, followed by AMD3100 or vehicle one hour before peripheral blood collection for CFU assays.
Voriconazole purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 14:2025.10.13.682145. [Abstract]
Experimental design for HSPC mobilization. Wild-type C57BL/6J or Townes SCD mice were treated with Voriconazole (50 mg/kg/day, iv) or vehicle intravenously daily for four days, followed by AMD3100 or vehicle one hour before peripheral blood collection for CFU assays. Numbers of CFU-C in peripheral blood of C57BL/6J mice after the indicated treatments.
Voriconazole purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 14:2025.10.13.682145. [Abstract]
Experimental design for HSPC mobilization. Wild-type C57BL/6J or Townes SCD mice were treated withVvoriconazole (50 mg/kg/day, iv) or vehicle intravenously daily for four days, followed by AMD3100 or vehicle one hour before peripheral blood collection for CFU assays. Numbers of CFU-gmEM (C) in peripheral blood of C57BL/6J mice after the indicated treatments.
Solvent & Solubility
DMSO : ≥ 50 mg/mL (143.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.17 mg/mL (0.49 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.16 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.16 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Nickie D Greer, et al. Voriconazole: the newest triazole antifungal agent.Proc (Bayl Univ Med Cent). 2003 Apr;16(2):241-8. [Content Brief]
[2]. Michael E Henry, et al. Quantification of brain voriconazole levels in healthy adults using fluorine magnetic resonance spectroscopy. Antimicrob Agents Chemother. 2013 Nov;57(11):5271-6. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8628 mL | 14.3139 mL | 28.6279 mL | 71.5697 mL |
| 5 mM | 0.5726 mL | 2.8628 mL | 5.7256 mL | 14.3139 mL | |
| 10 mM | 0.2863 mL | 1.4314 mL | 2.8628 mL | 7.1570 mL | |
| 15 mM | 0.1909 mL | 0.9543 mL | 1.9085 mL | 4.7713 mL | |
| 20 mM | 0.1431 mL | 0.7157 mL | 1.4314 mL | 3.5785 mL | |
| 25 mM | 0.1145 mL | 0.5726 mL | 1.1451 mL | 2.8628 mL | |
| 30 mM | 0.0954 mL | 0.4771 mL | 0.9543 mL | 2.3857 mL | |
| 40 mM | 0.0716 mL | 0.3578 mL | 0.7157 mL | 1.7892 mL | |
| 50 mM | 0.0573 mL | 0.2863 mL | 0.5726 mL | 1.4314 mL | |
| 60 mM | 0.0477 mL | 0.2386 mL | 0.4771 mL | 1.1928 mL | |
| 80 mM | 0.0358 mL | 0.1789 mL | 0.3578 mL | 0.8946 mL | |
| 100 mM | 0.0286 mL | 0.1431 mL | 0.2863 mL | 0.7157 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.