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Voriconazole P450 (e.g. CYP17) chemical

Name: Voriconazole
Brand: Selleck Chemicals
SKU: S1442
Rating: 5 (30 reviews)

Cat.No.S1442

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.

Chemical Structure

Molecular Weight: 349.31

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Dehydrogenase HSP Transferase PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other P450 (e.g. CYP17) Inhibitors	Apigenin Baicalein Avasimibe Naringenin Diosmetin Alizarin Orteronel Benzbromarone Sodium Danshensu Naringin

Chemical Information, Storage & Stability

Molecular Weight	349.31	Formula	C₁₆H₁₄F₃N₅O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	137234-62-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	UK-109496			Smiles	CC(C1=NC=NC=C1F)C(CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (200.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	P450
In vitro	Voriconazole is active against certain opportunistic filamentous and dimorphic Fungal (molds) and yeasts. This compound's 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. It inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates.
In vivo	Voriconazole is significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised guinea pigs with pulmonary aspergillosis. This compound also has been shown to be effective in guinea pigs with experimental pulmonary or intracranial infections caused by C. neoformans. This compound (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. It (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. This chemical (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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9431946/ [2] https://pubmed.ncbi.nlm.nih.gov/12904365/ [3] https://pubmed.ncbi.nlm.nih.gov/12121933/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	--

Tech Support

Handling Instructions

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Frequently Asked Questions

Question 1:
I am trying to use it 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:
It can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 8mg/ml clearly. When making the solution, please dissolve this compound in DMSO clearly first. Then add PEG and Tween, after they mixed well, then dilute with water.

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