1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. URAT1

URAT1

Urate transporter 1; SLC22A12

URAT1, a member of the OAT (organic anion transporter) family was first cloned from the human kidney, where it is localized to the apical (brush border) membrane of renal proximal tubular cells. URAT1 mediates the reabsorption of uric acid, thereby regulating blood uric acid concentrations. Impairment in URAT1 activity, either due to polymorphisms, or drug-drug interactions, can have toxicological consequences. In the kidney, URAT1 is distributed along the renal tubular cell membrane and involved in reabsorption and excretion of uric acid, organic acids, drugs and their metabolites. Uric acid is taken up by OAT1 and OAT3 from the blood and reabsorbed into renal tubular cells via URAT1, in exchange for dicarboxylic acid. URAT1, along with OAT4 mediates uptake of uric acid from the renal tubule into renal tubular cells in exchange for organic anions such as lactic acid and nicotinic acid. This exchange is electroneutral and can be trans-stimulated by Cl- gradients and gradients of lactate transported by the sodium-monocarboxylate transporter. In the salivary glands, URAT1 is distributed along the entire surface, including the ductal and acinar cells, suggesting a role in the transport of organic acids and uric acid in the whole salivary gland.

URAT1 Related Products (35):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162829
    hURAT1 inhibitor 1
    Inhibitor
    hURAT1 inhibitor 1 (compound 27b) is an isomarine-based, orally active dual hURAT1/GLUT9 inhibitor with IC50s of 0.16 μM and 4.47 μM, respectively, and has anti-hyperuricemia effects. hURAT1 inhibitor 1 showed significant uric acid-lowering activity in a hyperuricemia mouse model (10 mg/kg dose). hURAT1 inhibitor 1 had no significant in vitro cytotoxicity or in vivo hepatotoxicity and showed good PK characteristics.
    hURAT1 inhibitor 1
  • HY-153970
    URAT1 inhibitor 7
    Inhibitor
    URAT1 inhibitor 7 (compound 10f) is a potent URAT1 inhibitor, with an IC50 of 12 nM. URAT1 inhibitor 7 exhibits microsomal stability (HLM <13 µL/min/mg). URAT1 inhibitor 7 also inhibits CYP2C9, with an IC50 of 4.2 μM. URAT1 inhibitor 7 can be used for gout research.
    URAT1 inhibitor 7
  • HY-161523
    XOR/URAT1-IN-1
    Inhibitor
    XOR/URAT1-IN-1 (Compound II15) is a dual inhibitor for xanthine oxidoreductase (XOR) and uric acid transporter 1 (URAT1), with IC50 of 6 nM and 12.9 μM. XOR/URAT1-IN-1 lowers the levels of uric acid in Potassium oxonate (HY-17511)/Hypoxanthine (HY-N0091)-induced acute hyperuricemia mouse model.
    XOR/URAT1-IN-1
  • HY-152033
    URAT1 inhibitor 4
    Inhibitor
    URAT1 inhibitor 4, a Lesinurad derivative, is a potent and orally active URAT1 inhibitor with an IC50 of 7.56 μM. URAT1 inhibitor 4 has higher in vivo urate-lowering efficacy than Lesinurad (HY-15258).
    URAT1 inhibitor 4
  • HY-163431
    URAT1 inhibitor 10
    Inhibitor
    URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1 .
    URAT1 inhibitor 10
  • HY-159530
    Darbinuradum
    Darbinuradum (Darbinurad) is a urate transporter inhibitor.
    Darbinuradum
  • HY-143906
    URAT1 inhibitor 2
    Inhibitor
    URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout.
    URAT1 inhibitor 2
  • HY-153706
    URAT1 inhibitor 5
    Inhibitor
    URAT1 inhibitor 5 (compound 16) is a potent URAT1 inhibitor. URAT1 inhibitor 5 can be used in research of hyperuricemia.
    URAT1 inhibitor 5
  • HY-160265
    URAT1 inhibitor 9
    Inhibitor
    URAT1 inhibitor 9 (Compound 24) is an URAT1 inhibitor that can be used in the study of gout or hyperuricemia.
    URAT1 inhibitor 9
  • HY-15258S1
    Lesinurad-d4
    Inhibitor
    Lesinurad-d4 (RDEA594-d4) is deuterium labeled Lesinurad. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 μM, respectively.
    Lesinurad-d<sub>4</sub>
  • HY-168740
    URAT1 inhibitor 11
    Inhibitor
    URAT1 inhibitor 11 (Compound 7) is a URAT1 inhibitor with an IC50 value of 0.18 μM. URAT1 inhibitor 11 exhibits potent hypouricemic effects in hyperuricemic zebrafish induced by Potassium oxonate (HY-17511) and Xanthine sodium salt (HY-W017389).
    URAT1 inhibitor 11
  • HY-159581
    URAT1&XO inhibitor 3
    Inhibitor
    URAT1&XO inhibitor 3 (compound 27) is an orally active anti-gout agent targeting XO (IC50: 35 nM) and URAT1 (IC50: 31 nM). URAT1&XO inhibitor 3 has good pharmacological and pharmacokinetic (PK) characteristics and in vivo safety.
    URAT1&XO inhibitor 3
  • HY-157306
    HC-1310
    HC-1310 URAT1 Inhibitor (Compound 83) is a potent URAT1 inhibitor and can be used for research on hyperuricemia and gout.
    HC-1310
  • HY-111345A
    Epaminurad hydrochloride
    Inhibitor
    Epaminurad (UR-1102) hydrochloride is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a Ki of 0.057 μM. Epaminurad hydrochloride quite modestly inhibits OAT1 and OAT3 (organic anion transporter). Epaminurad hydrochloride is a uricosuric agent. Epaminurad hydrochloride can be used for gout and hyperuricemia research.
    Epaminurad hydrochloride
  • HY-W011711R
    Benzarone (Standard)
    Inhibitor
    Benzarone (Standard) is the analytical standard of Benzarone. This product is intended for research and analytical applications. Benzarone (Fragivix) is a potent human uric acid transporter 1 (hURAT1) inhibitor, with an IC50 of 2.8 μM in oocyte. Benzarone could lower uric acid serum levels.
    Benzarone (Standard)