Voriconazole
(Synonyms: 伏立康唑,(±)-UK-109496) 目录号 : GC13079
A triazole antifungal agent
Cas No.:137234-62-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Aspergillus spp. and Candida spp. |
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Preparation method |
The solubility of this compound in DMSO is >17.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Applications |
Voriconazole inhibited Aspergillus spp. and Candida spp. and exhibited excellent activity against Candida spp. with MICs typically <0.125 mg/L. |
| Clinical trial [2]: | |
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Patient models |
Aspergillosis |
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Application |
In the patients who received primary therapy with voriconazole, 59% had either a complete or a partial response. In the patients who received voriconazole as salvage therapy, 38% had either a complete or a partial response. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
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.
| Cas No. | 137234-62-9 | SDF | |
| 别名 | 伏立康唑,(±)-UK-109496 | ||
| 化学名 | (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1,2,4-triazol-1-yl)butan-2-ol | ||
| Canonical SMILES | CC(C1=NC=NC=C1F)C(CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O | ||
| 分子式 | C16H14F3N5O | 分子量 | 349.31 |
| 溶解度 | ≥ 34.9 mg/mL in DMSO, ≥ 45 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8628 mL | 14.3139 mL | 28.6279 mL |
| 5 mM | 0.5726 mL | 2.8628 mL | 5.7256 mL |
| 10 mM | 0.2863 mL | 1.4314 mL | 2.8628 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。