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L 006235

Cat. No. 3066

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Chemical Name: N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide

Biological Activity

Potent, reversible cathepsin K inhibitor (IC₅₀ = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. Displays reduced selectivity in cell-based assays possibly due to lysosomal accumulation. Reduces collagen breakdown and promotes bone deposition in vivo. Orally active and has intrinsic fluorescence.

Technical Data

M.Wt:

466.6

Formula:

C₂₄H₃₀N₆O₂S

Solubility:

Soluble to 100 mM in DMSO

Purity:

>98 %

Storage:

Store at +4°C

CAS No:

294623-49-7

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Falgueyret et al (2005) Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J.Med.Chem. 48 7535. PMID: 16302795.

Palmer et al (2005) Design and synthesis of tri-ring P₃ benamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J.Med.Chem. 48 7520. PMID: 16302794.

Desmarais et al (2008) Effects of cathepsin K inhibitors basicity on in vivo off-target activities. Mol.Pharmacol. 73 147. PMID: 17940194.

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