Xanthine oxidase-IN-4

Xanthine oxidase-IN-4 (compound 19a) is an orally active and potent xanthine oxidase (XO) inhibitor, with an IC50 of 0.039 μM. Xanthine oxidase-IN-4 exhibits hypouricemic potency in potassium oxonate induced hyperuricemia rats. Xanthine oxidase-IN-4 can be used for hyperuricemia and gout research[1].

Research Areas >> Metabolic Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Xanthine Oxidase

IC50: 0.039 μM (xanthine oxidase)[1]

Xanthine oxidase-IN-4 (compound 19a) (1 nM-10 μM, 15 min) exhibits a strong XO inhibitory potency, with an IC50 of 0.039 μM, and Ki of 0.0037 μM[1].

Xanthine oxidase-IN-4 (compound 19a) (SD rats, 10 mg/kg, Intragastrically, once) significantly reduces the serum concentration of uric acid[1]. Animal Model: Sprague-Dawley rats (Six weeks, male, 180-200g, six groups)[1] Dosage: 10 mg/kg Administration: Intragastrically, once Result: Significantly reduced the serum concentration of uric acid, with AUC (uric acid, 1-5 h) of 44.3%.

[1]. Zhao J, et al. Intramolecular hydrogen bond interruption and scaffold hopping of TMC-5 led to 2-(4-alkoxy-3-cyanophenyl)pyrimidine-4/5-carboxylic acids and 6-(4-alkoxy-3-cyanophenyl)-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-ones as potent pyrimidine-based xanthine oxidase inhibitors. Eur J Med Chem. 2022;229:114086.