Voriconazole
产品说明书
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同义名 : | UK-109496;DRG 0301;Vfend;VRC |
| CAS号 : | 137234-62-9 | |
| 货号 : | A615493 | |
| 分子式 : | C16H14F3N5O | |
| 纯度 : | 99% | |
| 分子量 : | 349.31 | |
| MDL号 : | MFCD00905717 | |
| 存储条件： |
Pure form Inert atmosphere,Store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
2% DMSO+30% PEG 300+2% Tween 80+water 8 mg/mL |
| 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]. | ||
| 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 << |
| 实验方案 | |||
|---|---|---|---|
| 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 |
| 参考文献 |
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