1. Membrane Transporter/Ion Channel
  2. URAT1
  3. URAT1 inhibitor 3

URAT1 inhibitor 3 

Cat. No.: HY-151432
Handling Instructions

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi.

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

URAT1 inhibitor 3 Chemical Structure

URAT1 inhibitor 3 Chemical Structure

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Description

URAT1 inhibitor 3 is a potent, orally active, selective URAT1 inhibitor with an IC50 value of 0.8 nM. URAT1 inhibitor 3 has urate-lowering efficacy. URAT1 inhibitor 3 can be used in research of gout and hyperuricemi[1].

IC50 & Target

IC50: 0.8 nM (URAT1)[1]

In Vitro

URAT1 inhibitor 3 (0-400 μM; 24 and 72 h; HepG2 and HK2 cells) has low toxicity and inhibits cell viability at high concentrations[1].
URAT1 inhibitor 3 (0.01-100 μM) has lower inhibition on urate excretion transporters with IC50 values of 10.16 μM and 4.04 μM of OAT1 and ABCG2, respectively[1].

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

Cell Viability Assay[1]

Cell Line: HepG2 and HK2 cells
Concentration: 0, 100, 200, 300, and 400 μM
Incubation Time: 24 and 72 hours
Result: Had little cytotoxicity at 24 h and inhibition rate of 34.75% and 35.9% of HepG2 and HK2 cells, respectively.
In Vivo

URAT1 inhibitor 3 (1-4 mg/kg; i.g.; once) has urate lowering efficacy in a mouse model of hyperuricemia[1].
URAT1 inhibitor 3 (50 mg/kg; i.g.; daily, for 14 d) has no hepatic and renal toxicities in mice[1].
URAT1 inhibitor 3 (50 mg/kg; i.g.; once) induces GSH depletion in Kunming mice with hyperuricemia model[1].

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

Animal Model: Male Kunming (KM) mice with hyperuricemia model[1]
Dosage: 1, 2, and 4 mg/kg
Administration: Oral gavage; once
Result: Decreased the serum urate levels in a dose-dependent manner.
Animal Model: Male Kunming mice[1]
Dosage: 50 mg/kg
Administration: Oral gavage; daily, for 14 days
Result: Did not cause renal toxicity.
Animal Model: Male Kunming mice with hyperuricemia model[1]
Dosage: 50 mg/kg
Administration: Oral gavage; once
Result: Decreased the serum GSH levels from 42.23 μM to 20.39 μM.
Molecular Weight

307.13

Formula

C14H8Cl2N2O2

SMILES

O=C(C1=CC(Cl)=C(O)C(Cl)=C1)N2C=CC3=CC=CN=C32

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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Product Name:
URAT1 inhibitor 3
Cat. No.:
HY-151432
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