The OAT (organic anion transporter) family member URAT1, which is restricted to the apical (brush border) membrane of renal proximal tubular cells, was first cloned from the human kidney. By mediating uric acid reabsorption, URAT1 controls blood uric acid concentrations. Toxicological effects may result from URAT1 activity impairment brought on by polymorphisms or drug-drug interactions. URAT1 is a protein that is found in the kidney and is involved in the reabsorption and excretion of uric acid, organic acids, drugs, and their metabolites. It is distributed along the renal tubular cell membrane. In exchange for dicarboxylic acid, uric acid is taken up by OAT1 and OAT3 from the blood and reabsorbed into renal tubular cells by URAT1.URAT1 and OAT4 facilitate uric acid uptake into renal tubular cells in exchange for organic anions like lactic acid and nicotinic acid in the renal tubule. This electroneutral exchange can be trans-stimulated by lactate gradients carried by sodium-monocarboxylate transporters as well as Cl- gradients. URAT1 is found throughout the surface of the salivary glands, including the ductal and acinar cells, suggesting that it plays a part in the transport of uric acid and other organic acids throughout the entire salivary gland.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V41641 | KPH2f | 2760615-09-4 | KPH2f is a novel, orally bioactive and potent dual URAT1/GLUT9 inhibitor with the potential to be used an anti-hyperuricemic agent for gout treatment. |
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V74201 | KPH2f | 2760615-09-4 | KPH2f is a safe, orally bioactive URAT1/GLUT9 dual (bifunctional) inhibitor, with IC50s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. |
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V3305 | Lesinurad | 878672-00-5 | Lesinurad (formerly RDEA-594; RDEA594;trade name: Zurampic)is a potent and selective URAT1(urate transporter 1) inhibitor approved as an anti-gout medication in 2016 by FDA. |
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V3306 | Lesinurad sodium | 1151516-14-1 | Lesinurad sodium (formerly known as RDEA594; RDEA-594; trade name Zurampic), thesodium salt of lesinurad, is a selective inhibitor ofURAT1(urate transporter 1) andOAT (organic anion transporter) approved in 2015 for treating high blood uric acid levels associated with gout. |
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V74254 | Lingdolinurad | 2088176-96-7 | Lingdolinurad is a uric acid transporter inhibitor that targets hURAT1. |
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V74247 | Ruzinurad (HR011303; SHR4640) | 1638327-48-6 | Ruzinurad (HR011303) is a selective URATl inhibitor (WO2020088641, compound I). |
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V74248 | URAT1 inhibitor 2 | 2803951-18-8 | URAT1 inhibitor 2 is an orally bioactive URAT1 and CYP isozyme inhibitor, with IC50s of 1.36 μM, 16.97 μM, and 5.22 μM for URAT1-mediated 14C-UA absorption, CYP1A2, and CYP2C9, respectively. |
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V74249 | URAT1 inhibitor 3 | 2850331-30-3 | URAT1 inhibitor 3 is an orally bioavailable and selective URAT1 inhibitor (antagonist) with IC50 of 0.8 nM. |
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V74198 | URAT1 inhibitor 4 | 2700292-02-8 | URAT1 inhibitor 4 is an analogue of Lesinurad and an orally bioactive URAT1 inhibitor (antagonist) with IC50 of 7.56 μM. |
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V74251 | URAT1 inhibitor 5 | 2102670-94-8 | URAT1 inhibitor 5 (compound 16) is a potent URAT1 inhibitor. |
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V74246 | URAT1 inhibitor 6 | 2244807-49-4 | URAT1 inhibitor 6 (Compound 1h) is a potent inhibitor of URAT1 (IC50 for hURAT1 is 35 nM). |
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V74250 | URAT1 inhibitor 8 | 1632005-33-4 | URAT1 inhibitor 8 (example 247) is a potent URAT1 inhibitor (antagonist) with IC50 of 0.001 μM. |
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V71985 | URAT1&XO inhibitor 2 | 1239488-96-0 | URAT1&XO inhibitor 2 (Compound BDEO) is a dual (bifunctional) inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. |
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V3308 | Verinurad (RDEA3170) | 1352792-74-5 | Verinurad (formerly known as RDEA-3170; RDEA3170) is a novel, highly potent and specificURAT1(Urate transporter 1) inhibitor with anti-hyperuricemic effects. |
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