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Voriconazole

In stock
Catalog No.
A4320
CYP51 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$50.00
In stock
25mg
$70.00
In stock
100mg
$105.00
In stock
200mg
$180.00
In stock

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Background

Voriconazole is an inhibitor of 14α-lanosterol demethylase with IC50 value of 53nM [1].

Voriconazole is a triazole antifungal and a second-generation synthetic derivative of fluconazole. It plays its antifungal role through inhibiting cytochrome P450 (CYP 450)–dependent 14α-lanosterol demethylation, which is a vital step in the membrane ergosterol synthesis of fungi. Voriconazole has a broad antifungal spectrum. It is active against all Candida species, many Aspergillus species and other yeasts, including Cryptococcus neoformans, Trichosporon beigelii, and Saccharomyces cerevisia. Voriconazole is available in both intravenous and oral formulations. Voriconazole undergoes extensive hepatic metabolism via the cytochrome P450 enzymes, primarily CYP2C9 and CYP3A4. In addition, voriconazole also causes some side effects, such as visual disturbances, skin rashes and elevations in hepatic enzyme levels [1, 2].

References:
[1] Sabo JA, Abdel-Rahman SM. Voriconazole: a new triazole antifungal. Ann Pharmacother. 2000 Sep;34(9):1032-43.
[2] Johnson LB, Kauffman CA. Voriconazole: a new triazole antifungal agent. Clin Infect Dis. 2003 Mar 1;36(5):630-7.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt349.31
Cas No.137234-62-9
FormulaC16H14F3N5O
Solubility≥34.9 mg/mL in DMSO, ≥45 mg/mL in EtOH with ultrasonic and warming, <2.5 mg/mL in H2O
Chemical Name(2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1,2,4-triazol-1-yl)butan-2-ol
SDFDownload SDF
Canonical SMILESCC(C1=NC=NC=C1F)C(CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Aspergillus spp. and Candida spp.

Preparation method

The solubility of this compound in DMSO is >17.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Applications

Voriconazole inhibited Aspergillus spp. and Candida spp. and exhibited excellent activity against Candida spp. with MICs typically <0.125 mg/L.

Clinical trial [2]:

Patient models

Aspergillosis

Application

In the patients who received primary therapy with voriconazole, 59% had either a complete or a partial response. In the patients who received voriconazole as salvage therapy, 38% had either a complete or a partial response.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Sabo JA, Abdel-Rahman SM. Voriconazole: a new triazole antifungal. Ann Pharmacother. 2000 Sep;34(9):1032-43.

[2] Johnson LB, Kauffman CA. Voriconazole: a new triazole antifungal agent. Clin Infect Dis. 2003 Mar 1;36(5):630-7.

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