RO5461111

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RO5461111

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1252637-46-9

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

RO5461111 是一种高特异性、口服有效的Cathepsin S拮抗剂 (IC₅₀: 0.4 nM, humanCathepsin S; 0.5 nM, murineCathepsin S)。RO5461111 能够有效抑制抗原特异性 T 细胞和 B 细胞活化。RO5461111 对肺部炎症和狼疮性肾炎有改善作用。

生物活性

RO5461111 a highly specific and orally active antagonist ofCathepsin SwithIC₅₀s of 0.4 nM (humanCathepsin S) and 0.5 nM (murineCathepsin 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].

IC₅₀& Target^[1]

human Cathepsin S

0.4 nM (IC₅₀)

murine Cathepsin S

0.5 nM (IC₅₀)

体外研究
(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]

体内研究
(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.

分子量

614.56

Formula

C₂₇H₂₄F₆N₄O₄S

CAS 号

1252637-46-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.