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ASP1617

Chemical Structure : ASP1617

CAS No.: 2241184-85-8

ASP1617 (ASP-1617)

Catalog No.: PC-22165Not For Human Use, Lab Use Only.

ASP1617 (ASP-1617) is a potent, highly specific and orally active cathepsin S (CatS) inhibitor with IC50 of 4.6 nM and 0.39 nM for human and mouse CatS, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ASP1617 (ASP-1617) is a potent, highly specific and orally active cathepsin S (CatS) inhibitor with IC50 of 4.6 nM and 0.39 nM for human and mouse CatS, respectively.
ASP1617 does not show significant activity for CatB, CatV, matriptase 2, and papain activities on a panel 61 different proteases.
ASP1617 induced invariant chain accumulation and decreased the expression level of MHC class ΙΙ on the cell surface in both mouse and human B cells.
ASP1617 prevented DO11.10 mice T cell proliferation to ovalbumin antigen.
Oral administration of ASP1617 suppressed anti-dsDNA IgG, prevented progression of lupus-like glomerulonephritis, and significantly prevented proteinuria excretion in SLE mouse model.

Physicochemical Properties

M.Wt 567.59
Formula C28H34F5N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-N-(1-Cyanocyclopropyl)-4-[difluoro[4-[(4-methyl-1-piperazinyl)methyl]-2-(trifluoromethyl)phenyl]methyl]-1-[(1-methylcyclopropyl)carbonyl]-2-pyrrolidinecarboxamide

References

1. Yuka Kawato, et al. Eur J Pharmacol. 2022 Mar 15:919:174826.

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