1. Membrane Transporter/Ion Channel
  2. URAT1 GLUT
  3. URAT1/GLUT9-IN-3

URAT1/GLUT9-IN-3 is an orally active URAT1/GLUT9 dual inhibitor with IC50 values of 4.01 and 1.60 μM. URAT1/GLUT9-IN-3 inhibits URAT1-mediated uric acid uptake and GLUT9-mediated uric acid transport, reducing renal urate reabsorption. URAT1/GLUT9-IN-3 reduces serum uric acid levels in hyperuricemic mice. URAT1/GLUT9-IN-3 can be used for the researches of gout and hyperuricemia.

For research use only. We do not sell to patients.

URAT1/GLUT9-IN-3

URAT1/GLUT9-IN-3 Chemical Structure

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Description

URAT1/GLUT9-IN-3 is an orally active URAT1/GLUT9 dual inhibitor with IC50 values of 4.01 and 1.60 μM. URAT1/GLUT9-IN-3 inhibits URAT1-mediated uric acid uptake and GLUT9-mediated uric acid transport, reducing renal urate reabsorption. URAT1/GLUT9-IN-3 reduces serum uric acid levels in hyperuricemic mice. URAT1/GLUT9-IN-3 can be used for the researches of gout and hyperuricemia[1].

IC50 & Target[1]

GLUT9

1.6 μM (IC50)

In Vitro

URAT1/GLUT9-IN-3 (Compound 17) potently inhibits human URAT1 with an IC50 of 4.01 μM[1].
URAT1/GLUT9-IN-3 potently inhibits GLUT9 with an IC50 of 1.60 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-∞ T1/2 Tmax Cmax CL F
Rat[1] 2 mg/kg i.v. 5380 ng·h/mL 5400 ng·h/mL 0.60 h 1.20 h 0.083 h 12100 ng/mL 374 mL/h/kg /
Rat[1] 20 mg/kg p.o. 18100 ng·h/mL 18200 ng·h/mL 3.20 h 1.70 h 2.33 h 4930 ng/mL / 33.71 %
In Vivo

URAT1/GLUT9-IN-3 (Compound 17) (0.5-2 mg/kg; p.o.) reduces serum uric acid levels in acute hyperuricemic mice by up to 82.4% at an oral dose of 2 mg/kg, with efficacy maintained at lower doses down to 0.5 mg/kg[1].
URAT1/GLUT9-IN-3 (1000 mg/kg; p.o.; single dose) shows no acute toxicity at an oral dose of 1000 mg/kg in healthy Kunming mice and exhibits favorable tolerance with no significant tissue damage following 14 days of daily oral dosing at 50 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Hyperuricemic mice (Male)[1]
Dosage: 0.5 mg/kg; 1 mg/kg; 2 mg/kg
Administration: p.o.
Result: Reduced serum uric acid (SUA) levels to 267 μM, corresponding to a decrease ratio (DR) of 82.1%.
Reduced SUA levels to 371 μM, corresponding to a DR of 70.2%.
Reduced SUA levels to 582 μM, corresponding to a DR of 47.6%.
Reduced SUA levels to 273 μM, corresponding to a DR of 82.4%.
Molecular Weight

653.63

Formula

C29H25BrN4O3S3

SMILES

O=C(CCCSC1=NC2=C(C(NC3=C4C(C=CC=C4)=C(C=C3)C5CC5)=N1)SC=C2)NS(C6=CC=C(C=C6)Br)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
URAT1/GLUT9-IN-3
Cat. No.:
HY-183658
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