hyperuricemia

Allopurinol (Zyloric) is a Xanthine Oxidase Inhibitor. The mechanism of action of allopurinol is as a Xanthine Oxidase Inhibitor.

Febuxostat (TEI 6720) is a xanthine oxidase inhibitor.

Nequinate is an anticoccidial agent, preventing coccidiosis .

Epaminurad HCl is a URAT1 inhibitor with partial inhibition of OAT1 and OAT3 (organic anion transporters).Epaminurad HCl is a pro-uric acid excretory agent used for the prevention and treatment of gout and hyperuricemia.

Irtemazole (R 60844) is a novel uricosuric substance that is valuable in the treatment of hyperuricemia and gout.

Lingdolinurad is a uric acid transporter protein inhibitor targeting hURAT1 for the study of hyperuricemia or gout.

Ethambutol dihydrochloride is an anti-mycobacterial compound that inhibits arabinosyl transferase activity to prevent cell wall formation and can be used to induce hyperuricemia models.

Fructose is a simple ketose monosaccharide widely found in many plants and commonly combines with glucose to form the disaccharide sucrose. It can be used to induce hyperuricemia and diabetes models.

Potassium oxonate is a uricase inhibitor that suppresses the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate and is commonly used to establish hyperuricemia models.

Adenine hydrochloride is a purine nucleobase and a chemical component of DNA and RNA. It is involved in cellular respiration, protein synthesis, and plays an important role in energy metabolism through high-energy molecules such as ATP, NAD, and FAD. It can be used to induce hyperuricemia and chronic kidney injury models.

Adenine hemisulfate is a purine-based nucleobase and an essential chemical component of DNA and RNA. It plays a key role in cellular respiration, the formation of ATP and coenzymes such as NAD and FAD, as well as in protein synthesis. It is commonly used to induce animal models of chronic liver and kidney injury and hyperuricemia.

Verinurad (RDEA3170) (RDEA3170) is an organic anion transporter URAT1 (SLC22A12) inhibitor for the treatment of gout and hyperuricemia.

Xanthine oxidoreductase-IN-3 is an orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 of 26.3 nM, suitable for use in acute hyperuricemia studies.

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.

URAT1 inhibitor 1 (1g) is a potent inhibitor of uric acid transporter 1 (URAT1) with an IC50 of 32 nM, and has potential therapeutic applications for treating hyperuricemia associated with gout.

Compound 27b, also known as hURAT1 inhibitor 1, is an isomarine-derived, orally active inhibitor that targets both hURAT1 and GLUT9 with IC50 values of 0.16 μM and 4.47 μM, respectively. This compound exhibits significant anti-hyperuricemia effects and has demonstrated potent uric acid-lowering activity in a hyperuricemia mouse model at a dose of 10 mg kg. Importantly, Compound 27b displays no notable in vitro cytotoxicity or in vivo hepatotoxicity, and possesses favorable pharmacokinetic (PK) characteristics.

CC15009 is a potent inhibitor of xanthine oxidoreductase (XOR), demonstrating an IC50 value of 0.237 nM. It effectively inhibits the oxidative subtype of XOR, thereby reducing the generation of the byproduct ROS and exhibiting antioxidant activity. CC15009 has shown a favorable dose-dependent uric acid-lowering effect in two different XOR substrate-induced hyperuricemia mouse models.

HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 μM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.

Xanthine oxidase-IN-16 is an effective orally active inhibitor of xanthine oxidase (XO), demonstrating significant therapeutic efficacy in rats with hyperuricemia and an IC50 of 102 nM.

URAT1 inhibitor11 (Compound 7) is a potent URAT1 inhibitor, exhibiting an IC50 of 0.18 μM. It effectively reduces uric acid levels in zebrafish with hyperuricemia induced by Potassium oxonate and Xanthinesodium salt.

hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC50 of 18 nM. It also exhibits some inhibitory activity against OATP1B1, with an IC50 of 0.73 μM. hURAT1 inhibitor 2 can be used in research related to hyperuricemia, gout, and other diseases associated with abnormal uric acid metabolism.

TRPV1 antagonist 10 is a potent, orally active TRPV1 antagonist with an IC50 of 33.06 nM and serves as a moderate to weak inhibitor of URAT1 (IC50 = 22.51 μM) and GLUT9 (inhibition of 60.25% at 50 μM). It exhibits analgesic and urate-lowering properties and is applicable for research in hyperuricemia and inflammatory pain.

Topiroxostat (FYX-051) is a selective xanthine oxidase inhibitor developed for the treatment and management of hyperuricemia and gout.

Epaminurad (UR-1102) is an orally active, potent, and selective URAT1 (urate transporter 1) inhibitor with a Ki of 0.057 μM, and it inhibits OAT1 and OAT3 (organic anion transporter) modestly. Epaminurad is a uricosuric agent used for research on gout and hyperuricemia [1].