urat1

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.

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.

Fraxin (Fraxoside) is a glucoside of fraxetin.

Puliginurad (YL-90148) is a potent and selective inhibitor of the urate transporter protein (URAT), effectively inhibiting uric acid reabsorption. It can be utilized for the prevention and treatment of 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.

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.

URAT1 inhibitor13 (compound 22k) is a potent inhibitor of URAT1, useful for research related to gout.

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].

URAT1 inhibitor 2 is an orally active inhibitor of URAT1 and CYP isozyme with IC50 values of 1.36 μM, 16.97 μM, and 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2, and CYP2C9, respectively [URAT1 inhibitor 2 is a promising drug candidate for the study of hyperuricemia and gout].

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 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].

Compound II15, known as XOR URAT1-IN-1, serves as 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 a mouse model of acute hyperuricemia induced by potassium oxonate and hypoxanthine.

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.

hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC50 of 18 nM. It also exhibits some inhibitory activity against OATP1B1, with an IC50 of 0.73 μM. hURAT1 inhibitor 2 can be used in research related to hyperuricemia, gout, and other diseases associated with abnormal uric acid metabolism.

Lingdolinurad is a uric acid transporter protein inhibitor targeting hURAT1 for the study of hyperuricemia or gout.

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.

TRPV1 antagonist 10 is a potent, orally active TRPV1 antagonist with an IC50 of 33.06 nM and serves as a moderate to weak inhibitor of URAT1 (IC50 = 22.51 μM) and GLUT9 (inhibition of 60.25% at 50 μM). It exhibits analgesic and urate-lowering properties and is applicable for research in hyperuricemia and inflammatory pain.

UNC569 (UNC 569) is a selective inhibitor of URAT1, a transporter in the kidney that regulates uric acid excretion from the body. It is also a selective uric acid re-absorption inhibitor. UNC569 could normalize the amount of uric acid excreted by gout patients previously classified as under-excretors.