urate transporter 1

Benzarone (Benzarona) is a potent inhibitor of human uric acid transporter 1 (URAT1, IC50 = 2.8 μM in oocyte). Benzarone lowers the level of uric acid serum.

Lesinurad (RDEA594) is a selective inhibitor of uric acid reabsorption which is used in combination with other agents in the therapy of gout. Lesinurad has had a limited clinical use but has not been associated with serum enzyme elevations during therapy or with instances of clinically apparent liver injury.

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

Dotinurad ((3,5-dichloro-4-hydroxyphenyl)(1,1-dioxidobenzo[d]thiazol-3(2H)-yl)methanone) is a potent agent of uricosuric (IC50: 3.6 μM for uric acid).

HNW005 is a dual inhibitor targeting the NLRP3 inflammasome and urate transporter 1 (URAT1). It exhibits an inhibition constant (KD) of 204.6 nM and an IC50 of 1.7 μM for NLRP3 inflammasome activation, while demonstrating an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. At an administered dose of 2 mg/kg in vivo, HNW005 achieves a uric acid reduction rate of 64.8%, effectively providing anti-inflammatory, analgesic, and urate-lowering effects by inhibiting NLRP3 inflammasome activation and uric acid transport. HNW005 is applicable for research in gouty arthritis.

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].