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Technical Data
| Formula | C22H17F2N5OS |
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| Molecular Weight | 437.47 | CAS No. | 241479-67-4 | |
| Solubility (25°C)* | In vitro | DMSO | 87 mg/mL (198.87 mM) | |
| Ethanol | 87 mg/mL (198.87 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Isavuconazole (BAL-4815, RO-0094815) is a new extended-spectrum triazole with activity against yeasts, molds, and dimorphic fungi that inhibits cytochrome P450 (CYP)-dependent 14α-lanosterol demethylation, which is essential for fungal cell membrane ergosterol synthesis. |
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| In vitro | 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[1]. |
| In vivo | 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[1]. |
Protocol (from reference)
Selleck's Isavuconazole has been cited by 1 publication
| Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Isavuconazonium Sulfate [ J Pharm Sci, 2023, 10.1016/j.xphs.2023.11.005] | PubMed: 37951471 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.