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Chemical Structure : Relacatib
Catalog No.: PC-62962Not For Human Use, Lab Use Only.
Relacatib (SB-462795, GSK-462795) is a potent and orally bioavailable small molecule cathepsin inhibitor with Ki of 41, 68 and 53 pM for cathepsin K, L and V, respectively.
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Relacatib (SB-462795, GSK-462795) is a potent and orally bioavailable small molecule cathepsin inhibitor with Ki of 41, 68 and 53 pM for cathepsin K, L and V, respectively.
Relacatib displays 39-300-fold selectivity over other cathepsins.
Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 of 45 nM and 70 nM, respectively.
Relacatib inhibits bone resorption both in vitro in human tissue and in vivo in cynomolgus monkeys.
| M.Wt | 540.635 | |
| Formula | C27H32N4O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yamashita DS, et al. J Med Chem. 2006 Mar 9;49(5):1597-612.
2. Kumar S, et al. Bone. 2007 Jan;40(1):122-31.
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