1252637-46-9
1252637-46-9 structure
- Name: RO5461111
- Chemical Name: RO5461111
- CAS Number: 1252637-46-9
- Molecular Formula: C27H24F6N4O4S
- Molecular Weight: 614.56
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Cathepsin
- Create Date: 2023-05-16 17:37:52
- Modify Date: 2024-02-03 23:45:53
-
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[1][2].
| Name | RO5461111 |
|---|
| Description | 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[1][2]. |
|---|---|
| Related Catalog | |
| Target |
human Cathepsin S:0.4 nM (IC50) murine Cathepsin S:0.5 nM (IC50) |
| In Vitro | 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 cells[1] |
| In Vivo | 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[1]。 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[1]。 Animal Model: Female MRL-Fas(lpr) mice (12-week-old; with proteinuria/serum creatinine levels up)[1] 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. |
| References |
| Molecular Formula | C27H24F6N4O4S |
|---|---|
| Molecular Weight | 614.56 |