Voriconazole
Catalog No.S1442 Synonyms: UK-109496
Molecular Weight(MW): 349.31
Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.
1 Customer Review
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Voriconazole increases the osteogenic activity of human osteoblasts in vitro. Osteoblasts were exposed to voriconazole (VCZ) or fluconazole (FCZ) at 15 or 200 μg/ml in osteoinductive medium (OS+) for up to 7 days. As a positive control, cells were also exposed to sodium fluoride (NaF) at 10 μM in nonosteoinductive medium (OS−). Osteoblastic differentiation was evaluated by measuring alkaline phosphatase (ALP) activity (A) and staining for calcium deposition with alazarin red S stain (B and C); calcium deposition was quantified by measuring the absorbance (A415) of extracted alazarin red S (B) and was assessed by the light microscopic appearance (white arrows) of stained osteoblast cultures (C). Values represent the means ± SD. *, P < 0.05, compared to osteoblasts grown under osteogenic conditions without treatment.
Antimicrob Agents Chemother, 2015, 59(12):7205-13.. Voriconazole purchased from Selleck.
Purity & Quality Control
Choose Selective P450 (e.g. CYP17) Inhibitors
Biological Activity
| Description | Voriconazole is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol. | |
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| Targets |
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| In vitro |
Voriconazole is active against certain opportunistic filamentous and dimorphic fungi (molds) and yeasts. Voriconazole in vitro activities are higher than or similar to those of itraconazole and amphotericin B for most of the molds tested, with the exceptions of R. arrhizus and S. schenckii. [1] Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates. [2] |
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| In vivo | Voriconazole is significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised guinea pig with pulmonary aspergillosis. Voriconazole also has been shown to be effective in guinea pigs with experimental pulmonary or intracranial infections caused by C. neoformans. [1] Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) significantly reduces the colony counts in the tissues of selected Guinea pigs compared with those in the tissues of the controls. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) also results in reductions in colony counts in tissues compared with those in the tissues of Guinea pigs treated with caspofungin acetate (the difference is not statistically significant) and improves the survival times but does not sterilize tissues. Voriconazole (5 mg/kg/day, i.p.) combined with caspofungin acetate (CAS) at either dose reduces colony counts in tissues 1,000-fold over those for the controls and are the only regimens that significantly reduces the numbers of positive cultures. [3] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 70 mg/mL (200.39 mM) |
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| Ethanol | 20 mg/mL (57.25 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing. |
8mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 349.31 |
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| Formula | C16H14F3N5O |
| CAS No. | 137234-62-9 |
| Storage | powder |
| in solvent | |
| Synonyms | UK-109496 |
Bio Calculators
Molarity Calculator
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00413218 | Completed | Candidiasis Invasive|Candidemia|Mycoses | Astellas Pharma Inc|Basilea Pharmaceutica | March 8 2007 | Phase 3 |
| NCT00412893 | Completed | Aspergillosis|Invasive Fungal Infection | Astellas Pharma Inc|Basilea Pharmaceutica International Ltd | March 7 2007 | Phase 3 |
| NCT02180165 | Completed | Aspergillosis | Merck Sharp & Dohme Corp. | July 29 2014 | Phase 3 |
| NCT01782131 | Recruiting | Fungal Infections | Merck Sharp & Dohme Corp. | September 25 2013 | Phase 3 |
| NCT01950507 | Completed | Stem Cell Transplantation|Graft vs Host Disease | National Institutes of Health Clinical Center (CC)|National Heart Lung and Blood Institute (NHLBI) | September 21 2013 | Phase 1 |
| NCT03672292 | Not yet recruiting | Invasive Pulmonary Aspergillosis | Scynexis Inc. | November 2018 | Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
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Question 1:
I am trying to use voriconazole in vivo via ip injection. Is the formulation recommended on your website (2% DMSO+30% PEG 300+2% Tween 80+ddH2O) suitable for injection?
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Answer:
S1442 can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 8mg/ml clearly. When making the solution, please dissolve the compound in DMSO clearly first. Then add PEG and Tween, after they mixed well, then dilute with water.
