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Voriconazole
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Voriconazole图片
CAS NO:137234-62-9
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)349.31
FormulaC16H14F3N5O
CAS No.137234-62-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 70 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 20 mg/mL (57.3 mM)
Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 10mg/mL
SynonymsUK-109496; UK 109496; Voriconazole; UK109496; UK109,496; UK-109,496; UK 109,496; Vfend

Chemical Name: (2R,3S)-2-(2,4-Difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol

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

SMILES Code: C[C@@H](C1=NC=NC=C1F)[C@@](O)(C2=CC=C(F)C=C2F)CN3N=CN=C3

实验参考方法
In Vitro

In vitro activity: 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. Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates


Cell Assay: Voriconazole(UK-109496) is a second-generation triazole antifungal used to treat serious fungal infections. IC50 Value: Target: Antifungal Voriconazole displays potent activity against Candida, Cryptococcus and Aspergillus species. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes.

In VivoVoriconazole 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. 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.
Animal modelGuinea pig
Formulation & Dosage1.25, 5 mg/kg/day, i.p.
References J Clin Microbiol. 1998 Jan;36(1):198-202; J Clin Microbiol. 2003 Aug;41(8):3623-6; Antimicrob Agents Chemother. 2002 Aug;46(8):2564-8.