
簡要描述:Isavuconazole 241479-67-4Isavuconazole(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557
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| 品牌 | absin | CAS | 241479-67-4 |
|---|---|---|---|
| 分子式 | C22H17F2N5OS | 純度 | >98% |
| 分子量 | 437.47 | 貨號 | abs47027985 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is the active component of the new azol | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Isavuconazole 241479-67-4
| 產(chǎn)品描述 | |
| 描述 | Isavuconazole(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557, exhibits MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabrata. |
| 純度 | >98% |
| 儲存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | 艾沙康唑; BAL-4815; RO-0094815 |
| 可溶性/溶解性 | DMSO : ≥ 50 mg/mL (114.29 mM) |
| 生物活性 | |
| 靶點 | Fungal |
| In vitro(體外研究) | Isavuconazole inhibits cytochrome P450 (CYP)–dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis. This blockade produces methylated sterols in the fungal membrane, altering its function and allowing the accumulation of ergosterol toxic precursors in the cytoplasm, which leads to cell death. |
| In vivo(體內(nèi)研究) | Isavuconazonium sulfate, the prodrug of isavuconazole, is available in both intravenous and oral formulations. After intravenous infusion, the prodrug is broken down quickly to the active component, isavuconazole, and an inactive cleavage product. Following oral administration, plasma concentrations of the active compound reach maximum concentrations (Cmax) by 2–3 hours; the prodrug and cleavage product are not measurable in plasma after oral administration. In healthy adult volunteers, isavuconazole exhibits linear and dose-proportional pharmacokinetics. The oral bioavailability of isavuconazole is 98%. Absorption of isavuconazole is not affected by food intake. In addition to excellent bioavailability, isavuconazole serum concentrations show low intersubject variability. In healthy volunteers, the Cmax at steady state was 2.5 ± 1.0 µg/mL. Isavuconazole has a large volume of distribution, is >99% protein bound, and has a long terminal half-life of 100-130 hours. Metabolism of isavuconazole takes place in the liver via the CYP enzyme family, specifically CYP3A4 and CYP3A5 isoenzymes. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | MetabolismTypes of disease Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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