Isavuconazole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。

Isavuconazole(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with 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.

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.

241479-67-4

C22H17F2N5OS

437.47

BAL-4815;RO-0094815;艾沙康唑

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years