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Based on 5 publication(s) in Google Scholar
Isavuconazole (BAL-4815) is a triazole proagent with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
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- 純度: 99.97%
- CAS 番号: 241479-67-4
- 分子式: C22H17F2N5OS
- 分子量:437.47
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Isavuconazole
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生物活性
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CYP3 |
Isavuconazole (BAL-4815) shows good activity against all Candida spp., with active MIC50 of 0.004 mg/L. The MIC50s/MIC90s range from 0.002/0.004 mg/L for C. albicans to 0.25/0.5 mg/L for C. glabrata[1]. Isavuconazole has potent in vitro activity against most common Aspergillus species, Purpureocillium lilacinum, and Scedosporium apiospermum[2]. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 μg/mL with others as high as 32 μg/mL[3]. In the study of pharmacokinetics and pharmacodynamics of isavuconazole against the GFP transformant, F/11628, NIH 4215, and F/16216, the modal MICs of isavuconazole are 1, 8, 1, 4 mg/L, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 241479-67-4
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性状 Solid
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分子量 437.47
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分子式 C22H17F2N5OS
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Color White to yellow
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SMILES
FC1=CC=C(F)C=C1[C@](CN2C=NC=N2)(O)[C@@H](C)C3=NC(C4=CC=C(C#N)C=C4)=CS3
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別名
Isavuconazole; BAL-4815; RO-0094815
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Drug Metab Dispos
A Systematic In Vitro Investigation of the Inhibitor Preincubation Effect on Multiple Classes of Clinically Relevant Transporters. [Abstract]2019 Jul;47(7):768-778. PMID: 31068368 -
Mycoses
COVID-19-associated pulmonary aspergillosis in ICU patients in a German reference centre: Phenotypic and molecular characterisation of Aspergillus fumigatus isolates. [Abstract]2022 Apr;65(4):458-465. PMID: 35138651 -
J Steroid Biochem Mol Biol
Molecular mechanisms of posaconazole- and itraconazole-induced pseudohyperaldosteronism and assessment of other systemically used azole antifungals. [Abstract]2020 May;199:105605. PMID: 31982514 -
溶剤 & 溶解度
DMSO : ≥ 50 mg/mL (114.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.71 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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参考文献
[1]. Seifert H, et al. In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates. Antimicrob Agents Chemother. 2007 May;51(5):1818-21. [Content Brief]
[2]. Steinmann J, et al. In Vitro Activity of Isavuconazole against Rasamsonia Species. Antimicrob Agents Chemother. 2016 Oct 21;60(11):6890-6891. [Content Brief]
[3]. Donnelley MA, et al. Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections. Infect Drug Resist. 2016 Jun 2;9:79-86. [Content Brief]
[4]. Box H, et al. Pharmacodynamics of Isavuconazole in a Dynamic In Vitro Model of Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2015 Oct 26;60(1):278-87. [Content Brief]
[5]. Livermore J, et al. Evaluation of the pharmacokinetics and clinical utility of isavuconazole for treatment of invasive fungal infections. Expert Opin Drug Metab Toxicol. 2012 Jun;8(6):759-65. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2859 mL | 11.4294 mL | 22.8587 mL | 57.1468 mL |
| 5 mM | 0.4572 mL | 2.2859 mL | 4.5717 mL | 11.4294 mL | |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2859 mL | 5.7147 mL | |
| 15 mM | 0.1524 mL | 0.7620 mL | 1.5239 mL | 3.8098 mL | |
| 20 mM | 0.1143 mL | 0.5715 mL | 1.1429 mL | 2.8573 mL | |
| 25 mM | 0.0914 mL | 0.4572 mL | 0.9143 mL | 2.2859 mL | |
| 30 mM | 0.0762 mL | 0.3810 mL | 0.7620 mL | 1.9049 mL | |
| 40 mM | 0.0571 mL | 0.2857 mL | 0.5715 mL | 1.4287 mL | |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4572 mL | 1.1429 mL | |
| 60 mM | 0.0381 mL | 0.1905 mL | 0.3810 mL | 0.9524 mL | |
| 80 mM | 0.0286 mL | 0.1429 mL | 0.2857 mL | 0.7143 mL | |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5715 mL |
Isavuconazole 関連分類
HY-14273 関連分類
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