RO5461111

Modify Date: 2024-02-03 23:45:53

RO5461111 structure	Common Name	RO5461111
	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 RO5461111

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	Research Areas >> Inflammation/Immunology Signaling Pathways >> Metabolic Enzyme/Protease >> Cathepsin
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	[1]. Rupanagudi KV, et al. Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming. Ann Rheum Dis. 2015 Feb;74(2):452-63. [2]. Sanchez RA, et al. Preparation of proline dipeptidyl nitrile derivatives as cathepsin, particularly cathepsin S and L, inhibitors: United States, US20100267722. 2010-10-21.

Molecular Formula	C₂₇H₂₄F₆N₄O₄S
Molecular Weight	614.56

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: RO5461111
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Purity: 98.0%
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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.