RO5461111
Modify Date: 2024-02-03 23:45:53
RO5461111 structure
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Common Name | RO5461111 | ||
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| CAS Number | 1252637-46-9 | Molecular Weight | 614.56 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C27H24F6N4O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RO5461111RO5461111 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]. |
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| 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 |
| InChIKey | CDBYZSRUFZXRLK-QUCCMNQESA-N |
| SMILES | Cc1cc(-c2ccc(S(=O)(=O)C3CC(C(=O)NC4(C#N)CC4)N(C(=O)C4(C(F)(F)F)CC4)C3)c(C(F)(F)F)c2)ccn1 |