Chemical Structure : RO5461111
CAS No.:
1252637-46-9
RO5461111
(RO-5461111, RO 5461111)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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614.56
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Formula
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C27H24F6N4O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2S,4R)-N-(1-Cyanocyclopropyl)-4-[[4-(2-methyl-4-pyridinyl)-2-(trifluoromethyl)phenyl]sulfonyl]-1-[[1-(trifluoromethyl)cyclopropyl]carbonyl]-2-pyrrolidinecarboxamide
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References
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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