Xanthine Oxidase Inhibitor

Xanthine oxidase-IN-24 is an orally active mixed-type inhibitor of xanthine oxidase, with an IC₅₀ of 0.051 μM and a K_i of 0.162 μM. Xanthine oxidase-IN-24 interacts with both free xanthine oxidase and the xanthine-xanthine oxidase complex, and reduces uric acid production in vivo. In a rat model of hyperuricemia induced by Potassium oxonate (HY-17511), Xanthine oxidase-IN-24 dose-dependently lowers serum uric acid levels, improves renal function-related biochemical parameters such as creatinine and urea nitrogen, and alleviates histopathological damage to liver and kidney tissues. Xanthine oxidase-IN-24 can be used in the research of hyperuricemia.

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.

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 agent-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.

Xanthine oxidase-IN-18 is a potent orally activeXanthine oxidase (XO) inhibitor (IC₅₀ = 0.263 μM). Xanthine oxidase-IN-18 exerts inhibition by directly and stably binding to the xanthine oxidase Mo-co active site. Xanthine oxidase-IN-18 exhibits reactive oxygen species (ROS) scavenging activity. Xanthine oxidase-IN-18 shows anti-hyperuricemia effects in a Potassium oxonate (HY-17511)-induced hyperuricemic rat model. Xanthine oxidase-IN-18 can be used for hyperuricemia, breast and lung cancer research.

Oxypurinol-¹³C₃,¹⁵N₃ (Oxipurinol-¹³C₃,¹⁵N₃) is the ¹³C- and ¹⁵N-labeled Oxypurinol (HY-19657). 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.

Forsythoside F (Arenarioside) is a xanthine oxidase inhibitor and possesses antihyperuricemic effects in vivo.

Xanthine oxidase-IN-17 is a potent xanthine oxidase (XOD) inhibitor with an IC₅₀ of 298 nM and a K_i of 167 nM. Xanthine oxidase-IN-17 decreases the formation of O_₂^⁻ radical by inhibiting the catalytic activity of XOD to diminish the production of uric acid. Xanthine oxidase-IN-17 shows no cytotoxicity in AML-12 hepatocytes, while suppressing uric acid production. Xanthine oxidase-IN-17 can be used for the studies of hyperuricemia and subsequently to gout.

Xanthine oxidase-IN-12 (Compound 11) is a xanthine oxidase (XO) inhibitor with an IC₅₀ of 91 nM. Xanthine oxidase-IN-12 also has antioxidant activity and reduces intracellular ROS.

XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC₅₀ of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model.

Eupatoriochromene is a chromene and has inhibitory activity against xanthine oxidase (XO).

Baicalein 6-O-glucoside is a glucuronidation metabolite of Baicalein.

Xanthine oxidase-IN-8 (Icarisids J) (Compound 7) is a XOD inhibitor with an IC₅₀ of 29.71 μM.

Angexostat (Compound 2) is an inhibitor of xanthine oxidase. Angexostat exhibits high permeability. Angexostat inhibits CYP2C9 with an IC₅₀ of 18.1 μM. Angexostat can be studied in research for xanthine oxidase-related diseases such as hyperuricemia and gout.

Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-type xanthine oxidase (XOD) inhibitor with an IC₅₀ value of 1.37 µM. Xanthine oxidase-IN-6 shows strong anti-hyperuricemia and renal protective activity.

XO/COX/LOX-IN-1 is a XO/COX/LOX inhibitor with an IC₅₀ of 3.2 μM against rat XO, 10.83 μM against 5-LOX, 12.67 μM against COX-1, and 8.31 μM against COX-2. XO/COX/LOX-IN-1 binds to the active sites of XO, 5-LOX, COX-1 and COX-2, thereby blocking enzyme activities associated with uric acid, leukotriene, prostaglandin synthesis and inflammatory pathways. XO/COX/LOX-IN-1 can be used in the research of hyperuricemia and inflammation.

Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor. Xanthine oxidoreductase-IN-4 has inhibitory activity against XOR with an IC₅₀ value of 29.3 nM. Xanthine oxidoreductase-IN-4 can be used for the research of hyperuricemia.

Ellagic acid 4-O-β-D-xylopyranoside is a natural ellagitannin with antimicrobial activity. Ellagic acid 4-O-β-D-xylopyranoside is an xanthine oxidase inhibitor with an ₅₀ of 2.1 μg/mL.

Xanthine oxidase-IN-10 (XO8 analog) is an xanthine oxidase (XO) inhibitor.

(+/-)-Epicatechin is a xanthine oxidase inhibitor with an IC₅₀ of 982.14 μM, and can be found in Semen Plantaginis (Plantago seed). (+/-)-Epicatechin can be used in research on diseases such as hyperuricemia and gout .

Tetrahydroamentoflavone (Amentoflavanone) is a potent xanthine oxidase (XO) inhibitor. Tetrahydroamentoflavone has inhibitory activity for XO with IC₅₀ and K_i values of 92 nM and 0.982 μM, respectively. Tetrahydroamentoflavone can be used for the research of inflammatory disorders and gout.