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Query String: FEBUXOSTAT

US9802907, Febuxostat BDBM352074
2-(3-CYANO-4-ISOBUTOXY-PHENYL)-4-METHYL-5-THIAZOLE-CARBOXYLIC ACID CHEMBL1164729 BDBM50320491 FEBUXOSTAT

?melcerovi?, A; Tomovi?, K; ?melcerovi?, ?; Petronijevi?, ?; Koci?, G; Toma?i?, T; Jakopin, ?; Anderluh, M Xanthine oxidase inhibitors beyond allopurinol and febuxostat; an overview and selection of potential leads based on in silico calculated physico-chemical properties, predicted pharmacokinetics and toxicity. Eur J Med Chem 135: 491-516 (2017)

Xanthine Oxidase (XO) Assay Xanthine oxidase (XO) assay of 2-(benzylamino)-4-methyl-1,3-thiazole-5-carboxylic acid derivatives 5a-p was evaluated using Bovine milk XO (grade 1, ammonium sulphate suspension, purchased by Sigma Aldrich). UV�visible spectrophotometer (EI 2371) was used for measuring uric acid formation at 293 nm at 25 �C under aerobic condition. The reaction mixture containing 1 mL xanthine (0.15 mM), 2.5 mL potassium phosphate buffer (50 mM, pH 7.4) and 0.5 mL of XO solution (0.405 U/mL) was incubated for 5 min at 25 �C. Inhibition of XO activity by various inhibitors was measured by following the decrease in the uric acid formation at 293 nM at 25 �C. The blank was prepared without enzyme solution. Febuxostat was used as positive control. The enzyme was preincubated for 5 min, with test compounds ranging from 6.25 to 100 �M (six concentrations in triplicate) dissolved in DMSO (1% v/v) (38,39), and the reaction started by the addition of xanthine. DMSO (1% v/v) did not interfere with the enzyme ac