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伏立康唑 /Voriconazole {[allProObj[0].p_purity_real_show]}

货号：A615493 同义名： UK-109496;DRG 0301

Voriconazole is a second-generation triazole antifungal used to treat serious fungal infections by inhibiting the synthesis of ergosterol, the major sterol of the fungal cell membrane.

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Voriconazole 化学结构 CAS号：137234-62-9
Voriconazole 化学结构
CAS号：137234-62-9
Voriconazole 3D分子结构
CAS号：137234-62-9
Voriconazole 化学结构 CAS号：137234-62-9
Voriconazole 3D分子结构 CAS号：137234-62-9
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Voriconazole 纯度/质量文件 产品仅供科研

货号：A615493 标准纯度： {[allProObj[0].p_purity_real_show]}
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Voriconazole 生物活性

描述 Cytochromes P450 (P450 or CYP) are heme-containing enzymes that catalyze the introduction of one atom of molecular oxygen into nonactivated C-H bonds, often in a regio- and stereoselective manner. This ability, combined with a tremendous number of accepted substrates, makes P450s powerful biocatalysts[3]. Voriconazole is extensively metabolized by the cytochrome P450 system with CYP2C19 being the major route for elimination[4]. Independent of the route of administration, voriconazole exposure was three times higher in CYP2C19 poor metabolizers compared with extensive metabolizers. Voriconazole has a high bioavailability with no large differences between the CYP2C19 genotypes. The hydroxylation pathway of voriconazole elimination exceeded the N-oxidation, both influenced by the CYP2C19 genotype[5]. Voriconazole is available for both oral and intravenous administration, it has broad-spectrum activity against pathogenic yeasts, dimorphic fungi and opportunistic moulds.Voriconazole has potent in vitro activity against Aspergillus spp., Fusarium spp. and Scedosporium apiospermum[6]. When orally administered, voriconazole increased the area under the plasma concentration-time curve (AUC), prolonged the elimination half-life (t1/2), and decreased the clearance (CL) of vonoprazan; there was no significant difference between the single-dose and multiple-dose groups. Voriconazole inhibited the metabolism of vonoprazan at an IC50 of 2.93 μM and showed mixed inhibition[7].

Voriconazole 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02381080 B-Cell Chronic Lymphocytic Leu... 展开 >>kemia 收起 << Phase 1 Completed - Canada ... 展开 >> N/a N/a, Canada Russian Federation Moscow, Russian Federation Petrozavodsk, Russian Federation St. Petersburg, Russian Federation Spain Madrid, Spain Pamplona, Spain 收起 <<
NCT00003031 Infection Pul... 展开 >>monary Complications 收起 << Phase 3 Completed - -
NCT01787032 Healthy Phase 1 Completed - Germany ... 展开 >> Boehringer Ingelheim Investigational Site Ingelheim, Germany 收起 <<

Voriconazole 参考文献

[1]Diekema DJ, Messer SA, et al. Activities of caspofungin, itraconazole, posaconazole, ravuconazole, voriconazole, and amphotericin B against 448 recent clinical isolates of filamentous fungi. J Clin Microbiol. 2003 Aug;41(8):3623-6.

[2]Espinel-Ingroff A. In vitro activity of the new triazole voriconazole(UK-109,496) against opportunistic filamentous and dimorphic fungi and common and emerging yeast pathogens. J Clin Microbiol. 1998 Jan;36(1):198-202.

[3]Vlada B Urlacher,et al. Cytochrome P450 Monooxygenases in Biotechnology and Synthetic Biology. Trends Biotechnol.2019 Aug;37(8):882-897.

[4]Mikus G, Scholz IM, Weiss J. Pharmacogenomics of the triazole antifungal agent voriconazole. Pharmacogenomics. 2011 Jun;12(6):861-72. doi: 10.2217/pgs.11.18.

[5]Scholz I, Oberwittler H, Riedel KD, et al. Pharmacokinetics, metabolism and bioavailability of the triazole antifungal agent voriconazole in relation to CYP2C19 genotype. Br J Clin Pharmacol. 2009 Dec;68(6):906-15. doi: 10.1111/j.1365-2125.2009.03534.x.

[6]Raoul Herbrecht. Voriconazole: therapeutic review of a new azole antifungal. Expert Rev Anti Infect Ther. 2004 Aug;2(4):485-97.

[7] Jiquan Shen,et al. Effects of Voriconazole on the Pharmacokinetics of Vonoprazan in Rats. Drug Des Devel Ther. 2020 Jun 4;14:2199-2206.

Voriconazole 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.63mL

5.73mL

2.86mL

Voriconazole 技术信息

CAS号137234-62-9
分子式C16H14F3N5O
分子量 349.31
别名 UK-109496;DRG 0301;Vfend;VRC
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(143.14 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

2% DMSO+30% PEG 300+2% Tween 80+water 8 mg/mL

Tags: Voriconazole | 137234-62-9 | UK-109496 | UK109496 | UK 109496 | Anti-infection | Fungal | Bacterial | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Voriconazole 纯度/质量文件 | Voriconazole 生物活性 | Voriconazole 临床数据 | Voriconazole 参考文献 | Voriconazole 实验方案 | Voriconazole 技术信息

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