产品
编 号:F743543
分子式:C27H24F6N4O4S
分子量:614.56
产品类型
结构图
CAS No: 1252637-46-9
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产品详情
生物活性:
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis.
体内研究:
RO5461111 (0.1-100 mg/kg; 口服; 单剂量) 可抑制 BALB/c 小鼠接种绵羊 IgG 后 T 细胞启动和抗绵羊 IgG。 RO5461111 (1.31 mg/mouse 或 30 mg/kg; 口服; 8 周) 破坏 MRL-Fas(lpr) 小鼠的生发中心 (如降低 CXCL12 表达),减少高丙种球蛋白血症和狼疮自身抗体产物 F。RO5461111 还可以减轻肺部炎症,改善狼疮性肾炎。Animal Model:Female MRL-Fas(lpr) mice (12-week-old; with proteinuria/serum creatinine levels up)
Dosage:262.5 mg/kg chow; or 5 mg/mouse with 1.31 mg/mouse
Administration:Oral gavage; 8 weeks
Result:Reduced the activation and expansion of spleen dendritic cells, CD4, double-negative T cells and plasma cells.Reduced plasma levels of IL-10 and TNF-α.
体外研究:
RO5461111 (16 h) is cytoactive in cell lines of human (RAJI) or mouse (A20), and significantly reduces splenic dendritic cell activation and subsequent expansion and activation of CD4 T cells and CD4/CD8 double negative T cellsRO5461111 相关抗体: