hyperuricemia

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.

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

Nequinate is an anticoccidial agent, preventing coccidiosis .

Febuxostat (TEI 6720) is a xanthine oxidase inhibitor.

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

Allopurinol Sodium is a xanthine oxidase inhibitor with an IC50 of 7.82±0.12 μM.

Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 29.3 nM, useful for studying 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 7 is a novel and potent inhibitor of the human uric acid transporter protein URAT1 (IC50:12 nM).URAT1 inhibitor 7 inhibits CYP2C9 with an IC50 of 4.2 μM.URAT1 inhibitor 7 can be used to study hyperuricemia and gout.

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.

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].

JTT-552, a uric acid transporter 1 (URAT1) inhibitor, is used potentially for the treatment of hyperuricemia.

LSPN451 is an effective xanthine oxidase inhibitor and may be used to treat hyperuricemia and gout.

Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)

Ruzinurad (WO2020088641, compound I) is a potent URAT1 inhibitor, exhibiting high selectivity. This compound shows great promise for investigating hyperuricemia.