产品
编 号:F763045
分子式:C14H8Cl2N2O2
分子量:307.13
产品类型
结构图
CAS No: 2850331-30-3
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产品详情
生物活性:
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.
体内研究:
URAT1 inhibitor 3 (1-4 mg/kg; i.g.; once) has urate lowering efficacy in a mouse model of hyperuricemia.URAT1 inhibitor 3 (50 mg/kg; i.g.; daily, for 14 d) has no hepatic and renal toxicities in mice.URAT1 inhibitor 3 (50 mg/kg; i.g.; once) induces GSH depletion in Kunming mice with hyperuricemia model.Animal Model:Male Kunming (KM) mice with hyperuricemia model
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
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
Dosage:50 mg/kg
Administration:Oral gavage; once
Result:Decreased the serum GSH levels from 42.23 μM to 20.39 μM.
体外研究:
URAT1 inhibitor 3 (0-400 μM; 24 and 72 h; HepG2 and HK2 cells) has low toxicity and inhibits cell viability at high concentrations.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.