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编 号:F754737
分子式:C27H20BrN3O4S3
分子量:626.56
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生物活性:
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).

体内研究:
URAT1 inhibitor 4 (2 mg/kg;单次口服) 降低急性高尿酸血症模型小鼠血清尿酸水平。URAT1 inhibitor 4 (1000 mg/kg; 单次灌胃) 在小鼠急性毒性评估中比 Lesinurad 的存活率更高。Animal Model:Kunming mice (acute?hyperuricemia?model)
Dosage:2 mg/kg
Administration:p.o.; single dosage
Result:Decreased serum uric acid with an decrease ratio of 73.29%.
Animal Model:Kunming mice
Dosage:1000 mg/kg
Administration:i.g.; single dosage
Result:Survival rate was 100% after 7 days, while Lesinurad were 40% (male) and 20% (female).

体外研究:
URAT1 inhibitor 4 (化合物 10) 抑制 URAT1 和 GLUT9,IC50 分别为 7.56 ± 0.52 μM 和 55.96 ± 10.38 μM。
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