URAT1

Total: 16
Updated: 2019-06-28 15:55:20
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.

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URAT1&XO inhibitor 1

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[1].

  • CAS Number: 2669726-78-5
  • MF: C20H13N5O3S
  • MW: 403.41
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Xininurad

Xininurad (XNW3009) is a urate transporter (URAT) inhibitor[1]

  • CAS Number: 2365178-28-3
  • MF: C15H10Br2FN3O2
  • MW: 443.07
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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URAT1 inhibitor 8

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[1].

  • CAS Number: 1632005-33-4
  • MF: C19H13ClFN3O4S
  • MW: 433.84
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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URAT1&XO inhibitor 2

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 Ki 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[1].

  • CAS Number: 1239488-96-0
  • MF: C14H12BrNO3
  • MW: 322.15
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Verinurad

Verinurad (RDEA3170) is a highly potent and specific URAT1 inhibitor with an IC50 of 25 nM[1].

  • CAS Number: 1352792-74-5
  • MF: C20H16N2O2S
  • MW: 348.418
  • Catalog: URAT1
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 566.7±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 296.5±30.1 °C
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URAT1 inhibitor 6

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[1].

  • CAS Number: 2244807-49-4
  • MF: C9H7BrN3NaO2S2
  • MW: 356.19
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Ruzinurad

Ruzinurad is a highly selective URATl inhibitor (WO2020088641, compound I). Ruzinurad can be used in the study of hyperuricemia[1].

  • CAS Number: 1638327-48-6
  • MF: C14H12BrNO2S
  • MW: 338.22
  • Catalog: URAT1
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 528.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 273.7±27.3 °C
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URAT1 inhibitor 1

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[1].

  • CAS Number: 2268720-62-1
  • MF: C19H15Br2N5O2S2
  • MW: 569.29
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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URAT1 inhibitor 7

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[1].

  • CAS Number: 1632002-28-8
  • MF: C19H10ClFN4O3S
  • MW: 428.82
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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URAT1 inhibitor 4

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)[1].

  • CAS Number: 2700292-02-8
  • MF: C27H20BrN3O4S3
  • MW: 626.56
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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URAT1 inhibitor 5

URAT1 inhibitor 5 (compound 16) is a potent URAT1 inhibitor. URAT1 inhibitor 5 can be used in research of hyperuricemia[1].

  • CAS Number: 2102670-94-8
  • MF: C18H14BrN3O2S
  • MW: 416.29
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Lingdolinurad

Lingdolinurad is urate transporter inhibitor, targeting to hURAT1.Lingdolinurad can be used for research in hyperuricemia in vitro and in vivo[1].

  • CAS Number: 2088176-96-7
  • MF: C17H12BrN3O2
  • MW: 370.20
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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UR-1102

Epaminurad (UR-1102) is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a Ki 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[1].

  • CAS Number: 1198153-15-9
  • MF: C14H10Br2N2O3
  • MW: 414.049
  • Catalog: URAT1
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 530.0±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 274.3±30.1 °C
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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.

  • CAS Number: 878672-00-5
  • MF: C17H14BrN3O2S
  • MW: 404.281
  • Catalog: URAT1
  • Density: 1.72±0.1 g/cm3
  • Boiling Point: 643.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 343.1±34.3 °C
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Lesinurad sodium

Lesinurad sodium 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.

  • CAS Number: 1151516-14-1
  • MF: C17H13BrN3NaO2S
  • MW: 426.26300
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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Puliginurad

Puliginurad (YL-90148) is a potent urate transporter (URAT) inhibitor. Puliginurad can be used for hyperuricemia and gout research[1].

  • CAS Number: 2013582-27-7
  • MF: C19H16N2O2S
  • MW: 336.41
  • Catalog: URAT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A
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