URAT1 inhibitor 4

Modify Date: 2023-01-14 19:43:11

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].

Name	URAT1 inhibitor 4

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	Signaling Pathways >> Membrane Transporter/Ion Channel >> URAT1 Research Areas >> Metabolic Disease
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.

Molecular Formula	C₂₇H₂₀BrN₃O₄S₃
Molecular Weight	626.56