Posaconazole
(Synonyms: 泊沙康唑; SCH 56592) 目录号 : GC17614
An antifungal agent
Cas No.:171228-49-2
Sample solution is provided at 25 µL, 10mM.
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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 |
25 strains of Coccidioides immitis |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
MIC: 0.5 μg/ml, 48 hours |
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Applications |
Posaconazole was tested in RPMI 1640 with L-glutamine and morpholinepropanesulfonic acid buffer at a concentration of 165 mM. The final concentration of the drug was 0.015 to 8 μg/ml. The MICs were read at 24 and 48 h. The posaconazole MICs ranged from 0.25 to 1 μg/ml, and the geometric mean posaconazole MIC was 0.5 μg/ml. The posaconazole MICs at which 50 of the isolates tested were inhibited (MIC50) and the MIC90 were 0.5 and 1 μg/ml, respectively. |
| Animal experiment: [2] | |
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Animal models |
Male BALB/c mice |
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Dosage form |
Oral administration, 5, 15, or 30 mg/kg twice per day, for 7 days |
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Applications |
Mice were rendered neutropenic with single doses of 5-fluorouracil and with cyclophosphamide one day before infection. This treatment reduced the neutrophil count. Mice were infected intravenously using a 0.2-ml volume of the inoculums. The antifungal agent treatment began 1 day after infection. The survival of posaconazole recipients increased significantly in a dose-dependent manner over that of the controls, with 60 to 83% survival at the 30-mg/kg twice-daily dose. Posaconazole doses of 15 and 30 mg/kg significantly lowered counts in tissue. Posaconazole at a dose of 30 mg/kg reduced many counts to undetectable levels. |
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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] González G M, Tijerina R, Najvar L K, et al. In vitro and in vivo activities of posaconazole against Coccidioides immitis. Antimicrobial agents and chemotherapy, 2002, 46(5): 1352-1356. [2] Sun Q N, Najvar L K, Bocanegra R, et al. In vivo activity of posaconazole against Mucor spp. in an immunosuppressed-mouse model. Antimicrobial agents and chemotherapy, 2002, 46(7): 2310-2312. | |
Posaconazole, also known as SCH 56592 or Noxafil, is a novel triazole antifungal compound that potently inhibits 14α-demethylation in a variety of fungi, including Candida (C. albicans C43, C. albicans C288, C. albicans C600 and C. albicans C248) and Aspergillus (A. fumigatus ND158 and A. flavus ND134), with half maximal inhibition concentration IC50 of 0.007 μg/ml, 0.06 μg/ml, 0.2 μg/ml, 0.3 μg/ml, 0.03 μg/ml and 0.03 μg/ml respectively [1].
Posaconzole, an itraconzole derivative with fluorine replacing chlorine in the phenyl ring and hydroxylation in the side chain, binds to the heme cofactor on the active site of 14α-demethylase, which converts lanosterol to 14α-dimethy lanosterol, resulting in the disruption of the integrity and function of the fungal cell membrane and inhibition of fungal growth [2].
References:
[1] Hanan K. Munayyer, Paul A. Mann, Andrew S. Chau, Taisa Yarosh-Tomaine, Jonathan R. Greene, Roberta S. Hare, Larry Heimark, Robert E. Palermo, David Loebenberg and Paul M. McNicholas. Posaconazole is a potent inhibitor of sterol 14α-demethylation in yeasts and molds. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY. 2004; 48(10): 3690-3696
[2] Daryl S. Schiller and Horatio B. Fung. Posaconazole: an extended-spectrum triazole antifungal agent. Clinical Therapeutics. 2007; 29(9): 1862-1886
| Cas No. | 171228-49-2 | SDF | |
| 别名 | 泊沙康唑; SCH 56592 | ||
| 化学名 | 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one | ||
| Canonical SMILES | CCC(C(C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5CC(OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F | ||
| 分子式 | C37H42F2N8O4 | 分子量 | 700.78 |
| 溶解度 | ≥ 35.039mg/mL in DMSO | 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 | 1.427 mL | 7.1349 mL | 14.2698 mL |
| 5 mM | 0.2854 mL | 1.427 mL | 2.854 mL |
| 10 mM | 0.1427 mL | 0.7135 mL | 1.427 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。