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

货号:A615493 同义名: UK-109496; DRG 0301

Voriconazole 是一种第二代三唑类抗真菌化合物,通过抑制麦角甾醇合成发挥抗真菌作用,常用于严重真菌感染的研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Voriconazole/伏立康唑 化学结构 CAS号:137234-62-9
Voriconazole/伏立康唑 化学结构
CAS号:137234-62-9
Voriconazole/伏立康唑 3D分子结构
CAS号:137234-62-9
Voriconazole/伏立康唑 化学结构 CAS号:137234-62-9
Voriconazole/伏立康唑 3D分子结构 CAS号:137234-62-9
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Voriconazole/伏立康唑 纯度/质量文件 产品仅供科研

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Voriconazole/伏立康唑 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/伏立康唑 细胞实验

Cell Line
Concentration Treated Time Description References
Rat liver microsomes 0.01, 0.1, 1, 10, 25, 50, 100 µM 50 minutes Voriconazole inhibited the metabolism of vonoprazan with an IC50 of 2.93 μM, showing mixed inhibition. Drug Des Devel Ther. 2020 Jun 4;14:2199-2206.
Candida albicans SC 5314 1.0 µg/mL To evaluate the antifungal activity of Voriconazole and its salts against Candida albicans Molecules. 2019 Oct 9;24(20):3635.
Candida glabrata DSM 11226 4.0 µg/mL To evaluate the antifungal activity of Voriconazole and its salts against Candida glabrata Molecules. 2019 Oct 9;24(20):3635.
Candida krusei DSM 6128 2.0 µg/mL To evaluate the antifungal activity of Voriconazole and its salts against Candida krusei Molecules. 2019 Oct 9;24(20):3635.
Candida tropicalis KKP 334 0.25 µg/mL To evaluate the antifungal activity of Voriconazole and its salts against Candida tropicalis Molecules. 2019 Oct 9;24(20):3635.
Candida lusitaniae DSM 70102 0.062 µg/mL To evaluate the antifungal activity of Voriconazole and its salts against Candida lusitaniae Molecules. 2019 Oct 9;24(20):3635.

Voriconazole/伏立康唑 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Sprague-Dawley rats Oral 30 mg/kg Single dose and multiple doses (14 days) To investigate the effects of voriconazole on the pharmacokinetics of vonoprazan, results showed that 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. Drug Des Devel Ther. 2020 Jun 4;14:2199-2206.

Voriconazole/伏立康唑 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/伏立康唑 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/伏立康唑 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/伏立康唑 技术信息

CAS号137234-62-9
分子式C16H14F3N5O
分子量 349.31
SMILES Code O[C@@]([C@@H](C)C1=NC=NC=C1F)(CN2N=CN=C2)C(C(F)=C3)=CC=C3F
MDL No. MFCD00905717
别名 UK-109496; DRG 0301; Vfend; VRC
运输蓝冰
InChI Key BCEHBSKCWLPMDN-VQVVDHBBSA-N
Pubchem ID 69155711
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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