URAT1 inhibitor 4

Modify Date: 2024-07-09 11:22:59

URAT1 inhibitor 4 Structure
URAT1 inhibitor 4 structure
Common Name URAT1 inhibitor 4
CAS Number 2700292-02-8 Molecular Weight 626.56
Density N/A Boiling Point N/A
Molecular Formula C27H20BrN3O4S3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of URAT1 inhibitor 4


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].

 Names

Name URAT1 inhibitor 4

 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

[1]. Zhang J, et al. Design, synthesis and activity evaluation of novel lesinurad analogues containing thienopyrimidinone or pyridine substructure as human urate transporter 1 inhibitors. Eur J Med Chem. 2022 Dec 15;244:114816.  

 Chemical & Physical Properties

Molecular Formula C27H20BrN3O4S3
Molecular Weight 626.56
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