Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
Voriconazole (UK-109496; UK109496; trade name Vfend) is a 2nd-generation and potent triazole-based antifungal drug used for treating a variety of fungal infections. It is structurally similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.
ln Vitro |
Strong action is shown by voriconazole against S. Apiospermum and C. neoformans, with 0.125-0.25 μg/mL and 0.5 μg/mL, respectively, as MICs[1]. The cytochrome P450 (CYP)-dependent enzyme 14-alpha-sterol demethylase is inhibited by voriconazole, which damages cell membranes and stops the growth of fungi [2].
|
---|---|
ln Vivo |
In a dose-dependent manner, voriconazole (5–20 mg/kg; orally for 21 days) extends survival. In the lungs, voriconazole (40 mg/kg/day) reduces the amount of fungal growth [3].
|
Animal Protocol |
Animal/Disease Models: Male specific-pathogen-free BALB/cByJ mice[3]
Doses: 1, 5, 20 mg/kg/day Route of Administration: Po one time/day for 21 days Experimental Results: Improved survival in a dose-response fashion, with median survival times (MSTs) of 21, 28, and 35 days with doses of 1, 5, and 20 mg/kg, respectively. |
References |
[1]. Nickie D Greer, et al. Voriconazole: the newest triazole antifungal agent.Proc (Bayl Univ Med Cent). 2003 Apr;16(2):241-8.
|
Molecular Formula |
C16H14F3N5O
|
---|---|
Molecular Weight |
349.31
|
CAS # |
137234-62-9
|
Related CAS # |
Voriconazole-d3;1217661-14-7;Voriconazole camphorsulfonate;137234-71-0
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C[C@@H](C1=NC=NC=C1F)[C@@](O)(C2=CC=C(F)C=C2F)CN3N=CN=C3
|
InChi Key |
BCEHBSKCWLPMDN-MGPLVRAMSA-N
|
InChi Code |
InChI=1S/C16H14F3N5O/c1-10(15-14(19)5-20-7-22-15)16(25,6-24-9-21-8-23-24)12-3-2-11(17)4-13(12)18/h2-5,7-10,25H,6H2,1H3/t10-,16+/m0/s1
|
Chemical Name |
(2R,3S)-2-(2,4-Difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
|
Synonyms |
UK-109496; UK 109496; Voriconazole; UK109496; UK109,496; UK-109,496; UK 109,496; Vfend
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.16 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol: 10mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8628 mL | 14.3139 mL | 28.6279 mL | |
5 mM | 0.5726 mL | 2.8628 mL | 5.7256 mL | |
10 mM | 0.2863 mL | 1.4314 mL | 2.8628 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05380245 | Completed | Drug: Voriconazole 200 mg x 2 Tablets Drug: Clarithromycin 500 mg x 1Tablets |
Healthy | Abdul Wali Khan University Mardan | November 1, 2018 | Phase 4 |
NCT01887457 | Suspended | Drug: VFEND | Aspergillosis Fusarium |
Brynn Chappell | September 2014 | Phase 2 |
NCT02110316 | Withdrawn | Other: Dosage form of voriconazole | Voriconazole Bioavailability |
University Medical Center Groningen | June 2015 | Phase 4 |
NCT01151085 | Completed Has Results | Drug: Voriconazole | Systemic Mycosis | Pfizer | April 2006 |