urat1 inhibitor 1

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.

URAT1&XO Inhibitor 1 (compound 29) serves as a dual inhibitor with IC50 values of approximately 10 μM for URAT1 and 1.01 μM for Xanthine Oxidase. It induces a hypouricemic effect in the potassium oxonate-induced hyperuricemic rat model and is utilized in research pertaining to hyperuricemia [1].

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.

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.

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.

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).

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.

URAT1 inhibitor 3 is a potent, orally active, selective inhibitor of URAT1 (IC50 = 0.8 nM) demonstrating urate-lowering efficacy, suitable for research in gout and hyperuricemia [1].

KPH2f, a dual URAT1 GLUT9 inhibitor, demonstrates safety, oral activity, and efficacy, with inhibitory concentrations (IC50s) of 0.24 μM for URAT1 and 9.37 μM for GLUT9. It exhibits minimal effects on OAT1 and ABCG2, with IC50 values of 32.14 μM and 26.74 μM, respectively [1].

URAT1 Inhibitor 4, derived from Lesinurad, is a potent, orally active inhibitor of URAT1 with an IC50 value of 7.56 μM, demonstrating greater in vivo urate-lowering efficacy than Lesinurad [1].

URAT1 Inhibitor 8 (example 247) serves as a highly potent inhibitor of URAT1, demonstrating an IC50 value of 0.001 μM. It is applicable in the study of gout [1].

URAT1 Inhibitor 5 (compound 16) serves as a powerful inhibitor of URAT1 and is utilized in hyperuricemia research [1].

URAT1 inhibitor 6 (Compound 1h), with an IC50 of 35 nM for hURAT1, demonstrates 200-fold and 8-fold greater potency compared to Lesinurad and Benzbromarone, respectively. This compound is utilized in the study of inflammation [1].

Compound BDEO (URAT1&XO inhibitor 2) serves as a dual-action inhibitor targeting both xanthine oxidase (XO) and URAT1, demonstrating an IC50 value of 3.3 μM for XO inhibition. It effectively impedes uric acid uptake in HEK293 cells with URAT1 expression, evidenced by a Ki of 0.145 μM. In hyperuricemic mice models, the compound has been shown to reduce serum urate levels and uric acid excretion, indicating potential utility for hyperuricemia research [1].

HC-1310 URAT1 Inhibitor (Compound 83) serves as a potent inhibitor of URAT1, suitable for studying hyperuricemia and gout [1].

URAT1 Inhibitor 9 (Compound 24) is utilized in the research of gout and hyperuricemia due to its inhibitory effects on URAT1 [1].