| Bioactivity | 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]. |
| Target | IC50: 7.56 ± 0.52 μM (URAT1), 55.96 ± 10.38 μM (GLUT9) |
| Invitro | 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: |
| Name | URAT1 inhibitor 4 |
| CAS | 2700292-02-8 |
| Formula | C27H20BrN3O4S3 |
| Molar Mass | 626.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |