URAT1 Inhibitor

Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor with an IC₅₀ of 25 nM.

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 µM, respectively.

Benzarone is an oral inhibitor of human urate transporter 1 (hURAT1) with an IC₅₀ value of 2.8 μM, and it also acts as an uncoupler of oxidative phosphorylation. Benzarone can cause liver damage and promote cell apoptosis and necrosis. Benzarone can be used to lower serum uric acid levels and for research in vascular diseases.

Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 μM, respectively.

Xininurad is a potent orally active URAT1 inhibitor with an IC₅₀ of 7.17 nM. Xininurad inhibits URAT1 activity to reduce serum uric acid levels and increase urinary uric acid excretion. Xininurad can be used for the research of hyperuricemia and gout.

URAT1/GLUT9-IN-3 is an orally active URAT1/GLUT9 dual inhibitor with IC₅₀ values of 4.01 and 1.60 μM. URAT1/GLUT9-IN-3 inhibits URAT1-mediated uric acid uptake and GLUT9-mediated uric acid transport, reducing renal urate reabsorption. URAT1/GLUT9-IN-3 reduces serum uric acid levels in hyperuricemic mice. URAT1/GLUT9-IN-3 can be used for the researches of gout and hyperuricemia.

URAT1/GLUT9-IN-2 is a selective, orally active URAT1/GLUT9 inhibitor, with an IC₅₀ of 2.81 μM against URAT1 and an IC₅₀ of 12.53 μM against GLUT9. URAT1/GLUT9-IN-2 reduces serum uric acid levels and protects renal function. URAT1/GLUT9-IN-2 can be used in research related to hyperuricemia and hyperuricemic nephropathy.

URAT1-IN-16 is an orally active URAT1 inhibitor with an IC₅₀ value of 0.19 μM. URAT1-IN-16 also functions as an NLRP3 inflammasome pathway inhibitor by effectively suppressing mature IL-1β secretion (IC₅₀ = 2.52 μM). URAT1-IN-16 exhibits remarkable serum uric acid-lowering and anti-inflammatory activities in vivo, and can be used for hyperuricemia and gout research.

KPH2f is a safe, orally active, and effective dual URAT1/GLUT9 inhibitor with IC₅₀s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. KPH2f shows little effects on OAT1 and ABCG2 (IC₅₀=32.14 and 26.74 μM).

URAT1 inhibitor 8 (example 247) is a potent URAT1 inhibitor, with an IC₅₀ of 0.001 μM. URAT1 inhibitor 8 can be used for gout research.

URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC₅₀ of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.

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

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC₅₀ value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.

Ruzinurad (HR011303) is a highly selective URATl inhibitor (WO2020088641, compound I). Ruzinurad can be used in the study of hyperuricemia.

Puliginurad (YL-90148) is a potent urate transporter (URAT) inhibitor. Puliginurad can be used for hyperuricemia and gout research.

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

URAT1 inhibitor 6 (Compound 1h) is a potent URAT1 inhibitor (IC₅₀: 35 nM for hURAT1). URAT1 inhibitor 6 is 200- and 8-fold more potent than parent Lesinurad (HY-15258) and Benzbromarone (HY-B1135). URAT1 inhibitor 6 can be used for research of inflammation.

URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC₅₀=~10 μM) and Xanthine Oxidase (IC₅₀=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research.

URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC₅₀ of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a K_i value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia.

hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC₅₀ of 18 nM. hURAT1 inhibitor 2 also has a certain inhibitory effect on OATP1B1, with an IC₅₀ value of 0.73 μM. hURAT1 inhibitor 2 can be used in the research of diseases related to abnormal uric acid metabolism, such as hyperuricemia and gout.