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Voriconazole (UK-109496)

Name: Voriconazole (UK-109496)
Brand: Selleck Chemicals
SKU: S1442
Rating: 5 (19 reviews)

Catalog No.S1442

For research use only.

Voriconazole (UK-109496) 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 (UK-109496) Chemical Structure

CAS No. 137234-62-9

Selleck's Voriconazole (UK-109496) has been cited by 19 publications

Purity & Quality Control

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P450 (e.g. CYP17) Signaling Pathway Map

Biological Activity

Description

Targets

P450 ^[1]

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

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 (from reference)

References

Solubility (25°C)

In vitro


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. Click to purchase: PEG300 Tween 80	8mg/mL

Chemical Information

Molecular Weight	349.31
Formula	C₁₆H₁₄F₃N₅O
CAS No.	137234-62-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC(C1=NC=NC=C1F)C(CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04865419	Recruiting	Drug: AZD0466\|Drug: Voriconazole	Haematological Malignancies	AstraZeneca	June 11 2021	Phase 1\|Phase 2
NCT04824417	Recruiting	Drug: Itraconazole 200 mg\|Drug: Voriconazole 200mg	Chronic Pulmonary Aspergillosis	Postgraduate Institute of Medical Education and Research	March 1 2021	Phase 3
NCT04229303	Completed	Drug: Voriconazole inhaled\|Drug: oral voriconazole	Allergic Bronchopulmonary Aspergillosis	Zambon SpA	February 11 2020	Phase 1
NCT04743544	Recruiting	Drug: Voriconazole	Adverse Drug Reactions	Dokuz Eylul University\|University of Liverpool	November 1 2019	--

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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