URAT1 inhibitor 4
Names
[ CAS No. ]:
2700292-02-8
[ Name ]:
URAT1 inhibitor 4
Biological Activity
[Description]:
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].
[Related Catalog]:
[Target]
IC50: 7.56 ± 0.52 μM (URAT1), 55.96 ± 10.38 μM (GLUT9)[1]
[In Vitro]
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[1]。
[In Vivo]
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[1]。 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)[1] 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[1] 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).
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C27H20BrN3O4S3
[ Molecular Weight ]:
626.56