Bioactivity | URAT1 inhibitor 10 (Compound 23a) is a URAT1 inhibitor. URAT1 inhibitor 10 has oral efficacy and low cytotoxicity. URAT1 inhibitor 10 has high selectivity for OAT1 [1]. |
Invitro | URAT1 inhibitor 10 (5 μM; 30min) 在 MDCK-hOAT 细胞中对 OAT1 的活性抑制(IC50 =9.17 μM)[1]。URAT1 inhibitor 10 (24 h) 在 RAW264.7 细胞中,对 IL-6 有中度抑制作用 (IR = 25.6%),可能缓解与 MSU 晶体介导的炎性细胞因子相关的症状[1]。URAT1 inhibitor 10 对 HepG2 细胞显示低细胞毒性 (IC50 > 64 μg/mL)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> URAT1 inhibitor 10 相关抗体: |
In Vivo | URAT1 inhibitor 10 (50 mg/kg; p.o.) 具有良好的药代动力学特性[1]。URAT1 inhibitor 10 (10 mg/kg; p.o.一天一次持续七天) 用氧酸钾诱导的高尿酸血症小鼠模型中,血清尿酸 (SUA) 显示出显着的活性降低,降低比率为 53.9 %, 相当于相同剂量下的阳性对照 Lesinurad (HY-15258)[1]。Pharmacokinetic Analysis in URAT1 inhibitor 10 Model[1] 药代动力学分析[1] Route |
CAS | 3012586-38-5 |
Formula | C19H20F3N3O3S |
Molar Mass | 427.44 |
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]. Li S et al. Proline-derived quinoline formamide compounds as human urate transporter 1 inhibitors with potent uric acid-lowering activities. Eur J Med Chem. 2024 Apr 5;269:116327 |