艾沙康唑 T2305

Product Introduction
Bioactivity


英文名: Isavuconazole

描述: Isavuconazole (RO-0094815) 是一种三唑类前药，对酵母、霉菌和二型真菌具有抗真菌活性。它抑制麦角固醇生物合成，导致真菌膜结构和功能的破坏。它是 CYP3A4抑制剂。

激酶实验: SP2509 activity assays: Test compounds are diluted to 20 × the desired test concentration in 100% DMSO and 2.5?μL of the diluted drug sampleis added to a black 384-well plate. The LSD1 enzyme stock is diluted 17-fold with assay buffer and 40?μL of the diluted LSD1 enzyme is added to the appropriate wells. Substrate, consisting of horseradish peroxidase, dimethyl K4 peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3, and 10-acetyl-3,7-dihydroxyphenoxazine is then added to wells. Resorufin is analyzed on an Envision plate reader with an excitation wavelength of 530?nm and an emission wavelength of 595?nm. The activity of SP2509 on the other oxidases is determined by using commercially available kits. The glucose oxidase activity (which also noncovalently binds FAD in an elongate conformation), is determined using the glucose oxidase kit. The MAO assays are performed using the MAO-glo kit with MAO-A and MAO-B.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 70 mg/mL (160.01 mM)


关键字: prodrug | dimorphic | Inhibitor | ergosterol | Antibiotic | Isavuconazole | CYPs | RO 0094815 | triazole | BAL4815 | biosynthesis | Fungal | fungi | RO0094815 | yeasts | inhibit | BAL 4815 | Cytochrome P450 | molds

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相关库: Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Fluorochemical Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Metabolism Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途