URAT1

Xininurad is a selective urate transporter (URAT) inhibitor that modulates uric acid levels in the body. By inhibiting URAT, it promotes renal excretion of uric acid, making it a valuable tool for studying hyperuricemia and related conditions such as gout. This compound serves as a potential therapeutic agent in research aimed at understanding and treating disorders associated with elevated urate concentrations.

URAT1 inhibitor 3 is a selective inhibitor of the urate transporter 1 (URAT1), demonstrating a potent inhibition with an IC50 value of 0.8 nM. This compound effectively lowers urate levels, making it valuable for studies focused on gout and hyperuricemia. Its oral bioavailability allows for convenient administration in various biological assays and preclinical research settings.

Ruzinurad is a highly selective inhibitor of the URAT1 transporter, which plays a critical role in the regulation of uric acid levels. By inhibiting URAT1, Ruzinurad effectively reduces uric acid reabsorption, making it a valuable tool in the study of hyperuricemia and related metabolic disorders. This compound has potential applications in research focusing on conditions such as gout and other diseases associated with elevated uric acid levels.

Puliginurad is a potent inhibitor of the urate transporter (URAT), which plays a critical role in uric acid reabsorption in the renal system. This compound is valuable for research in hyperuricemia and gout, offering insights into uric acid metabolism and potential therapeutic interventions. Its application in experimental studies can help elucidate the mechanisms underlying these conditions and support the development of novel treatment strategies.

URAT1 inhibitor 6 is a selective inhibitor of the urate transporter URAT1, exhibiting an IC50 value of 35 nM for human URAT1. This compound demonstrates significantly enhanced potency compared to its parent compound, Lesinurad, and the reference compound Benzbromarone. URAT1 inhibitor 6 is valuable for investigating uric acid transport and inflammation-related research applications.

URAT1 inhibitor 8 is a potent inhibitor of the urate transporter URAT1, exhibiting an IC50 of 0.001 μM. This compound is valuable for research applications focused on gout, offering insights into mechanisms of uric acid regulation and potential therapeutic strategies for hyperuricemia. Its high efficacy makes it a significant tool for studying renal handling of urate and related disorders.

URAT1&XO Inhibitor 1 is a dual inhibitor targeting both URAT1 and Xanthine Oxidase, with IC50 values of approximately 10 μM and 1.01 μM, respectively. This compound effectively induces a hypouricemic effect in a potassium oxonate-induced hyperuricemia rat model. URAT1&XO Inhibitor 1 is valuable for research applications focused on hyperuricemia and related disorders.

URAT1&XO Inhibitor 2 is a dual inhibitor targeting xanthine oxidase and URAT1, exhibiting an IC50 of 3.3 μM for xanthine oxidase. This compound effectively inhibits uric acid uptake in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. In hyperuricemic mouse models, it has been shown to reduce serum urate levels and decrease uric acid excretion. URAT1&XO Inhibitor 2 is valuable for researching conditions related to hyperuricemia.

hURAT1 inhibitor 2 is a selective inhibitor of hURAT1 (uric acid transporter 1, SLC22A12), exhibiting an IC50 of 18 nM. Additionally, it demonstrates moderate inhibitory activity on OATP1B1 with an IC50 of 0.73 μM. This compound is valuable for research focused on disorders associated with dysregulated uric acid metabolism, including hyperuricemia and gout.

Lingdolinurad is a selective inhibitor of the urate transporter URAT1. It effectively reduces urate reabsorption, making it a valuable tool in studying hyperuricemia. This compound can be applied in both in vitro and in vivo research to explore its potential therapeutic effects and underlying mechanisms in disorders associated with elevated uric acid levels.

JTT-552 is a selective URAT1 inhibitor known for its ability to reduce uric acid reabsorption in the renal system. This compound demonstrates significant potential in managing hyperuricemia and treating gout by promoting uric acid excretion. Its application in research can aid in understanding the pathophysiology of gout and developing therapeutics aimed at uric acid regulation.

URAT1 inhibitor 7 is a potent inhibitor of the urate transporter URAT1, demonstrating an IC50 of 12 nM. This compound exhibits excellent microsomal stability, with a hepatic microsomal clearance rate of less than 13 µL/min/mg. Additionally, it has been shown to inhibit CYP2C9 with an IC50 of 4.2 µM. URAT1 inhibitor 7 is suitable for research applications focused on gout and related disorders.

XOR/URAT1-IN-1 is a dual inhibitor targeting xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), exhibiting IC50 values of 6 nM and 12.9 μM, respectively. This compound effectively reduces uric acid levels in models of acute hyperuricemia induced by potassium oxonate or hypoxanthine. It serves as a valuable tool for studying disorders related to hyperuricemia and offers potential therapeutic insights for conditions such as gout.

URAT1 Inhibitor 10 is a potent inhibitor of the URAT1 transporter, demonstrating high selectivity for OAT1. This compound exhibits oral bioavailability and low cytotoxicity, making it suitable for in vivo studies. It is primarily used in research applications focused on renal physiology and uric acid transport, aiding investigations into gout and related disorders.

Darbinuradum is an inhibitor of the urate transporter URAT1, primarily impacting uric acid reabsorption in the renal proximal tubule. This compound demonstrates significant potential in research related to hyperuricemia and gout management by reducing uric acid levels in plasma. It is utilized in studies investigating the therapeutic effects of urate-lowering therapies and their implications for cardiovascular health and kidney function.

URAT1 inhibitor 13 is a selective inhibitor of the urate transporter 1 (URAT1), which is primarily involved in renal urate reabsorption. This compound exhibits strong biological activity in reducing urate levels and is particularly relevant in the study of gout and other related hyperuricemia conditions. Researchers can utilize URAT1 inhibitor 13 to explore its therapeutic potential and the underlying mechanisms in urate regulation.

URAT1 inhibitor 2 is a potent inhibitor of the URAT1 transporter, exhibiting an IC50 of 1.36 µM for URAT1-mediated 14C-UA uptake, alongside effective inhibition of CYP1A2 and CYP2C9 with IC50 values of 16.97 µM and 5.22 µM, respectively. This compound demonstrates significant potential in the investigation of hyperuricemia and gout, making it a valuable tool for biochemical research and therapeutic development.

URAT1 Inhibitor 5 is an effective inhibitor of the urate transporter URAT1. This compound has demonstrated potential in modulating uric acid reabsorption, making it relevant for the investigation of hyperuricemia and related conditions. Its application in biochemical research can facilitate the development of therapeutics targeting disorders associated with elevated uric acid levels.

URAT1 Inhibitor 9 targets the urate transporter URAT1, playing a crucial role in regulating uric acid levels. This compound demonstrates significant biological activity in the management of gout and hyperuricemia by inhibiting uric acid reabsorption in the kidneys. URAT1 Inhibitor 9 is valuable for research focusing on urate homeostasis and associated metabolic disorders.

URAT1 Inhibitor 11 is a potent inhibitor of the URAT1 transporter, exhibiting an IC50 value of 0.18 μM. This compound demonstrates significant hypouricemic effects in hyperuricemic zebrafish models induced by potassium oxonate and xanthine sodium salt. URAT1 Inhibitor 11 serves as a valuable tool for research applications focused on hyperuricemia and related metabolic disorders.

URAT1&XO Inhibitor 3 is a potent inhibitor of both xanthine oxidase (XO) and urate transporter 1 (URAT1), with IC50 values of 35 nM and 31 nM, respectively. This compound exhibits significant potential as an orally active anti-gout agent, demonstrating favorable pharmacological and pharmacokinetic properties. Additionally, URAT1&XO Inhibitor 3 has been shown to have in vivo safety, making it a valuable tool for research in the management of hyperuricemia and gout-related disorders.

HC-1310 is a potent inhibitor of URAT1, a transporter involved in uric acid reabsorption in the renal system. This compound is primarily utilized in research focused on hyperuricemia and gout, providing valuable insights into therapeutic strategies for managing elevated uric acid levels. By inhibiting URAT1, HC-1310 facilitates increased uric acid excretion, making it a critical tool for studying conditions associated with abnormal purine metabolism.

URAT1-IN-14 is a potent inhibitor of the urate transporter 1 (URAT1), demonstrating a human URAT1 inhibition IC50 of 0.72 μM in HEK293 cells. This compound exhibits minimal cytotoxicity in Hep-G2 cells, making it suitable for cellular applications. URAT1-IN-14 has been shown to effectively reduce urate levels in hyperuricemia mouse models, supporting its use in research related to hyperuricemia and gout.