xanthine

Xanthine (Isoxanthine) is a product on the pathway of purine degradation. Xanthine is subsequently converted to uric acid by the action of the Xanthine oxidase enzyme. Xanthine is found in most body tissues and fluids in various organisms. Biologically Xanthine is produced from guanine by cypin (guanine deaminase). Furthermore, Xanthines act as antagonists for adenosine receptors, with selectivity depending on whether there are substitution of alkyl groups.

Xanthine amine congener trihydrochloride is a potent adenosine antagonist that reverses the reduction in urine flow, sodium excretion and heart rate produced by the adenosine agonist, N6-cyclohexyladenosine.

Xanthine oxidoreductase-IN-5 is an orally active inhibitor of xanthine oxidoreductase (XOR) with an IC50 of 55 nM. Xanthine oxidoreductase-IN-5 may be used in studies of acute hyperuricemia.

Xanthine oxidase-IN-10 (XO8 analog) is an inhibitor of xanthine oxidase (XO) used in gout research.

Xanthine oxidase-IN-15 (Compound 6c) is a selective inhibitor of Xanthine oxidase (XO) with an IC50 of 0.13 μM. It inhibits XO by forming stable interactions at the enzyme's active site. Xanthine oxidase-IN-15 is primarily utilized in research related to hyperuricemia and gout.

Xanthine oxidase-IN-13 (Compound 10) is a selective inhibitor of xanthine oxidase, with an IC50 of 149.56 μM for bovine xanthine oxidase. It is utilized in the study of inflammatory arthritis.

Xanthine oxidase-IN-17 is a potent xanthine oxidase (XOD) inhibitor with an IC50 of 298 nM and a Ki of 167 nM. By inhibiting the catalytic activity of XOD, it reduces uric acid production and subsequently decreases the formation of O₂⁻ free radicals. Xanthine oxidase-IN-17 is non-cytotoxic in AML-12 liver cells while effectively inhibiting uric acid formation. It is suitable for research on hyperuricemia and gout.

Xanthine oxidase-IN-18 is a potent orally bioavailable xanthine oxidase (XO) inhibitor with an IC50 of 0.263 μM. It exerts its inhibitory effects by directly and stably binding to the Mo-co active site of xanthine oxidase. Xanthine oxidase-IN-18 also possesses reactive oxygen species (ROS) scavenging capabilities. In a potassium oxonate-induced hyperuricemia rat model, it exhibits antihyperuricemic effects. This compound is applicable in research related to hyperuricemia, breast cancer, and lung cancer.

Xanthine oxidase-IN-21, a Genipin derivative, is an orally effective mixed competitive inhibitor of xanthine oxidase (XOD) with an IC50 of 0.68 μM. It alleviates renal fibrosis by reducing α-SMA expression and modulates the NF-κB pathway to inhibit pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. Additionally, Xanthine oxidase-IN-21 suppresses the expression of URAT1 and GLUT9, promoting uric acid excretion and lowering serum uric acid levels. This compound exhibits significant hepatorenal protective effects and can be used in research on hyperuricemia.

Xanthine oxidase-IN-20 is a potent and orally active xanthine oxidase (XO) inhibitor, with an IC50 of 1.7 nM. In mouse and rat models of acute hyperuricemia, it significantly reduces serum uric acid (SUA) levels. Xanthine oxidase-IN-20 exhibits good safety and is applicable in research on hyperuricemia and gout.

Xanthine oxidase-IN-22 is an orally active inhibitor of xanthine oxidase (XO) with an IC50 value of 0.0034 μM. It exhibits a mixed-type inhibition mode against XO and effectively reduces serum uric acid levels in mice. Xanthine oxidase-IN-22 is applicable for research related to hyperuricemia and gout.

Xanthine oxidase-IN-23 (Compound BPF) is an orally active, reversible, mixed-type inhibitor of xanthine oxidase with an IC50 of 3.33 μM. It directly binds to XOD in a reversible mixed-type manner, inhibiting its catalytic activity. Additionally, Xanthine oxidase-IN-23 increases ABCG2 and decreases GLUT9 expression to facilitate renal uric acid excretion. This compound reduces serum uric acid levels and improves kidney function in hyperuricemic mice, making it useful for hyperuricemia research.

Xanthine amine congener is an Adenosine receptor antagonist.

Xanthine amine congener dihydrochloride (XAC dihydrochloride), a potent antagonist for both Adenosine A1 and A2 receptors with IC50 values of 1.8 nM for A1 and 114 nM for A2, also functions as a convulsant agent in mouse models.

Xanthine oxidase-IN-7 (compound 1h) is a potent, orally active xanthine oxidase (XO) inhibitor with an IC50 of 0.36 μM, effectively reducing serum uric acid levels and showing potential for hyperuricemia and gout research [1].

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

Xanthine oxidoreductase-IN-1 is a xanthine oxidoreductase (XOR) inhibitor with an IC 50 value of 7.0 nM.

Xanthine oxidase-IN-5, a powerful and orally active inhibitor of xanthine oxidase (XO), exhibits an IC50 value of 0.70 μM. It possesses favorable drug-like characteristics, with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Moreover, Xanthine oxidase-IN-5 showcases significant hypouricemic effects in a hyperuricemic rat model [1].

Xanthine oxidoreductase-IN-2 (Compound IVa) is a potent xanthine oxidoreductase (XOR) inhibitor, with an IC50 value of 7.2 nM, demonstrating hypouricemic effects in mice as evidenced by [1].

Xanthine amine congener (XAC) hydrochloride, a non-selective adenosine receptor antagonist, induces convulsions in mice.

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

Xanthine oxidase-IN-8 (Icarisids J) (Compound 7) acts as an inhibitor of xanthine oxidase with an inhibitory concentration (IC50) of 29.71 μM [1].

Xanthine Oxidase-IN-9 (also known as Icarisids E or Compound 2) effectively inhibits xanthine oxidase (XOD) with an IC50 value of 31.81 μM [1].

Xanthine oxidase (XO) is an enzyme involved in purine catabolism and conversion to uric acid, generating reactive oxygen species, used in the study of cardiovascular diseases.