| Identification | Back Directory | [Name]
Acetamide, N-[(4-bromophenyl)sulfonyl]-2-[[3-(4-cyclopropyl-1-naphthalenyl)-3,4-dihydro-4-oxothieno[2,3-d]pyrimidin-2-yl]thio]- | [CAS]
2700292-02-8 | [Synonyms]
URAT1 inhibitor 4
Acetamide, N-[(4-bromophenyl)sulfonyl]-2-[[3-(4-cyclopropyl-1-naphthalenyl)-3,4-dihydro-4-oxothieno[2,3-d]pyrimidin-2-yl]thio]- | [Molecular Formula]
C27H20BrN3O4S3 | [MOL File]
2700292-02-8.mol | [Molecular Weight]
626.56 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
URAT1 inhibitor 4 (2 mg/kg; p.o.; single dosage) decreases serum uric acid level in acute hyperuricemia model mice[1].
URAT1 inhibitor 4 (1000 mg/kg; i.g.; single dosage) exhibits higher survival rate than Lesinurad in mice acute toxicity assessment[1]. | 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. DOI:10.1016/j.ejmech.2022.114816 |
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