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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Cathepsin-RO5461111
RO5461111

Chemical Structure : RO5461111

CAS No.: 1252637-46-9

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RO5461111 (RO-5461111, RO 5461111)

货号: PC-22164Not For Human Use, Lab Use Only.

RO5461111 is a potent, highly specific and orally active cathepsin S (CatS) inhibitor with IC50 of 0.4 nM and 0.5 nM for human and mouse CatS respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RO5461111 is a potent, highly specific and orally active cathepsin S (CatS) inhibitor with IC50 of 0.4 nM and 0.5 nM for human and mouse CatS respectively.
RO5461111 significantly reduced the activation of spleen dendritic cells and the subsequent expansion and activation of CD4 T cells and CD4/CD8 double-negative T cells.
RO5461111 impaired the spatial organisation of germinal centres, suppressed follicular B cell maturation to plasma cells and Ig class switch.
Oral administration of RO5461111r (approximately 1.31 mg/day, stable plasma concentration of 400–600 ng/ml) protected MRL-Faslpr mice, which spontaneously develop SLE and lupus nephritis, from severe disease.

物理化学性质&存储条件

分子量 614.56
分子式 C27H24F6N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(2S,4R)-N-(1-Cyanocyclopropyl)-4-[[4-(2-methyl-4-pyridinyl)-2-(trifluoromethyl)phenyl]sulfonyl]-1-[[1-(trifluoromethyl)cyclopropyl]carbonyl]-2-pyrrolidinecarboxamide

参考文献

1. Rupanagudi KV, et al. Ann Rheum Dis. 2015 Feb;74(2):452-63.

2. Choi E, et al. Cancer Sci. 2024 Apr 13. doi: 10.1111/cas.16174.

3. Nicholas J. Bernard. Nature Reviews Rheumatology volume 10, page66 (2014).

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