Xanthine oxidoreductase-IN-3 is an orally active xanthine oxidoreductase (XOR) inhibitor, with an IC50 of 26.3 nM. Xanthine oxidoreductase-IN-3 can be used for the research of acute hyperuricemia[1].
Xanthine oxidoreductase-IN-2 (Compound IVa) is a xanthine oxidoreductase (XOR) inhibitor with the IC50 of 7.2 nM. Xanthine oxidoreductase-IN-2 shows hypouricemic effects in mice[1].
Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.Target: XAOAllopurinol (Zyloprim, and generics) is a drug used primarily to treat hyperuricemia (excess uric acid in blood plasma) and its complications, including chronic gout. It is a xanthine oxidase inhibitor which is administered orally. A common misconception is that allopurinol is metabolized by its target, xanthine oxidase, but this action is principally carried out by Aldehyde oxidase. The active metabolite of allopurinol is oxypurinol, which is also an inhibitor of xanthine oxidase. Allopurinol is almost completely metabolized to oxypurinol within two hours of oral administration, whereas oxypurinol is slowly excreted by the kidneys over 18–30 hours. For this reason, oxypurinol is believed responsible for the majority of allopurinol's effect.Allopurinol is a purine analog; it is a structural isomer of hypoxanthine (a naturally occurring purine in the body) and is an inhibitor of the enzyme xanthine oxidase. In addition to blocking uric acid production, inhibition of xanthine oxidase causes an increase in hypoxanthine and xanthine. While xanthine cannot be converted to purine ribotides, hypoxanthine can be salvaged to the purine ribotides adenosine and guanosine monophosphates. Increased levels of these ribotides may cause feedback inhibition of amidophosphoribosyl transferase, the first and rate-limiting enzyme of purine biosynthesis. Allopurinol, therefore, decreases uric acid formation and may also inhibit purine synthesis.
Forsythoside F (Arenarioside) is a xanthine oxidase inhibitor and possesses antihyperuricemic effects in vivo[1].
URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC50=~10 μM) and Xanthine Oxidase (IC50=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research[1].
Myricetin 3-O-galactoside, isolated from the leaves of Myrtus communis, inhibits xanthine oxidase (XO) activity, lipid peroxidation and scavenges the free radical. Myricetin 3-O-galactoside inhibits lipid peroxidation with an IC50 of 160 μg/mL. Antioxidant activity[1].
Febuxostat-d7 is deuterium labeled Febuxostat. Febuxostat (TEI 6720) is selective xanthine oxidase inhibitor with a Ki of 0.6 nM[1].
Ilexoside O is a triterpene saponin isolated from the roots of Ilex pubescens. Ilexoside O exhibits weak xanthine oxidase (XOD) inhibitory activity (IC50=53.05 μM)[1].
6-Formylpterin is an inhibitor of Xanthine Oxidase. 6-Formylpterin induces intracellular ROS generation and apoptosis in HL-60 cells. 6-Formylpterin suppresses cell proliferation in PanC-1 cells[1].
O-Desisobutyl-O-n-propyl Febuxostat, extracted from the patent CN 103467412, is an xanthine oxidase inhibitor[1].
Benzbromarone is a highly effective and well tolerated non-competitive inhibitor of xanthine oxidase, used as an uricosuric agent, used in the treatment of gout.
Tetrahydroamentoflavone (Amentoflavanone) is a potent xanthine oxidase (XO) inhibitor. Tetrahydroamentoflavone has inhibitory activity for XO with IC50 and Ki values of 92 nM and 0.982 μM, respectively. Tetrahydroamentoflavone can be used for the research of inflammatory disorders and gout[1].
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways[1][2].
Prudomestin, isolated from the heartwood of Prunus domestica, shows potent xanthine oxidase (XO) inhibitory activity (IC50≈6 µM)[1][2].
Xanthine oxidase-IN-1 is a xanthine oxidase inhibitor extracted from patent WO2008126898A1, page 68, compound example 3, with an IC50 of 6.5 nM.
Febuxostat (TEI 6720) sodium is a potent, selective and non-purine xanthine oxidase (XO) inhibitor with a Ki value of 0.6 nM. Febuxostat sodium has the potential for the research of hyperuricemia and gout[1][2][3].
Morin 3-O-β-D-glucopyranoside is a natural flavonoid with antifungal, anticancer and antioxidant activities. Morin 3-O-β-D-glucopyranoside inhibits reverse transcriptase, protein-tyrosine kinase and xanthine oxidase, and also shows anti-HIV, antiarteriosclerotic, and superoxide scavenging activities[1].
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells[1][2][3][4].
Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout[1].
Febuxostat acyl glucuronide (Febuxostat acyl-β-D-glucuronide) is a metabolite of Febuxostat (HY-14268). Febuxostat is a potent, selective and non-purine xanthine oxidase (XO) inhibitor[1].
7,8,3′,4′-Tetrahydroxyflavone (compound 2) is a potent xanthine oxidase (XOD) inhibitor with an IC50 value of 10.488 µM[1].
Tigulixostat is a novel (indolyl)heteroarylcarboxylate derivatives effective as non-purine selective xanthine oxidase inhibitor, which lowers the production of uric acid[1].
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].
Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.IC50 value: 5.3 nM [1]Target: xanthine oxidoreductasein vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3].in vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2].
Xanthine oxidase-IN-8 (Icarisids J) (Compound 7) is a XOD inhibitor with an IC50 of 29.71 μM[1].
Baicalein 6-O-glucoside is a glucuronidation metabolite of Baicalein[1].
Flazin is a non-enzymatic protein glycation inhibitor, also inhibits peroxynitrite (ONOO-), with an IC50 value of 85.31 μM for bovine serum albumin (BSA) glycation and an EC50 value of 71.99 μM for ONOO-. Flazin can be used for researching diabetes and neuronal disorders. Flazin also can used as a lipid droplet (LD) regulator against lipid disorders, and a xanthine oxidase (XOD) inhibitor[1][2][3].
Broussoflavonol F possess xanthine oxidase inhibitory activity[1].
Nequinate, a quinoline compound, is an anticoccidial agent against cecal coccidiosis (Eimeria tenella) infections[1]. Nequinate inhibits xanthine oxidoreductase (XOD) activity[2].
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable drug-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model[1].