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Voriconazole

现货
Catalog No.
A4320
CYP51抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
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10mg
¥ 500.00
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25mg
¥ 700.00
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100mg
¥ 1,050.00
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200mg
¥ 1,800.00
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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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

曲霉属和念珠菌属

溶解方法

在DMSO中的溶解度>17.5mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

应用

Voriconazole抑制曲霉属和念珠菌属,并表现出对念珠菌属的极好活性,MIC通常<0.125mg/L。

临床试验[2]:

疾病模型

曲霉菌病

应用

在接受Voriconazole初次治疗的患者中,59%具有完全或部分反应。 在接受Voriconazole治疗作为补救疗法的患者中,38%有完全或部分反应。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

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.

质量控制

化学结构

Voriconazole