Small-molecule inhibitor: relacatib
Name
- Common name
- relacatib
- Other names
- SB-462795
Inhibition
- History
- The discovery of relacatib arose from a study of structure-activity relationships in a series of azepanone inhibitors (Yamashita et al., 2006).
- Peptidases inhibited
- Relacatib inhibits cathepsin K with 0.5 nM IC50. In whole cell assays, cathepsin B, cathepsin L and cathepsin S were inhibited with similar potency, whereas odanacatib proved more selective for cathepsin K (Gauthier et al., 2008).
- Pharmaceutical relevance
- Relacatib showed potential as a drug for control of bone resorption when it preserved cortical and cancellous bone mass in ovariectomized monkeys (Stroup, Kumar & Jerome, 2009).
Chemistry
- CID at PubChem
- 6918602
- Structure
![[relacatib (C01.036 inhibitor) structure ]](http://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&cid=6918602)
Properties
- Synthesis
- Wang et al., 2008; Wang et al., 2009; Goodman et al., 2011
