Home Metabolism P450 (e.g. CYP17) chemical - Fungal chemical Voriconazole For research use only.

Voriconazole

Synonyms: UK-109496

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.

Voriconazole Chemical Structure

Voriconazole Chemical Structure

CAS No. 137234-62-9

Purity & Quality Control

Voriconazole Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

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.
Targets
P450 [1]
In vitro
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]
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04865419 Terminated
Haematological Malignancies
AstraZeneca
 June 11 2021 Phase 1|Phase 2
NCT04824417 Active not recruiting
Chronic Pulmonary Aspergillosis
Post Graduate Institute of Medical Education and Research Chandigarh|PGIMER
 March 1 2021 Phase 3
NCT04229303 Completed
Allergic Bronchopulmonary Aspergillosis
Zambon SpA
 February 11 2020 Phase 1
NCT04743544 Unknown status
Adverse Drug Reactions
Dokuz Eylul University|University of Liverpool
 November 1 2019 --

Chemical Information & Solubility

Molecular Weight 349.31 Formula

C16H14F3N5O
CAS No. 137234-62-9 SDF Download Voriconazole SDF
Smiles CC(C1=NC=NC=C1F)C(CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (200.39 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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Frequently Asked Questions

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?

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.

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