362505-84-8
Chemical Structure
Relacatib
Synonym(s): SB-462795
- CAS No.: 362505-84-8
- Formula:C27H32N4O6S
- Molecular Weight:540.63
IUPAC Name: N-((S)-4-methyl-1-(((4S,7R)-7-methyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)amino)-1-oxopentan-2-yl)benzofuran-2-carboxamide
InChIKey: BWYBBMQLUKXECQ-GIVPXCGWSA-N
SMILES: O=C(C1=CC2=CC=CC=C2O1)N[C@H](C(N[C@@H]3C(CN(S(=O)(C4=NC=CC=C4)=O)[C@H](C)CC3)=O)=O)CC(C)C
Biological Activity: Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Relacatib | 99.58% | Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo. | ||||||||||||||||||||
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Relacatib (Standard) | ≥98% | Relacatib (Standard) is the analytical standard of Relacatib (HY-10294). This product is intended for research and analytical applications. Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo. | ||||||||||||||||||||
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- [1]. Dennis S Yamashita, et al. Structure Activity Relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one Cathepsin K Inhibitors.J Med Chem [Content Brief]
- [2]. S Kumar, et al.A Highly Potent Inhibitor of Cathepsin K (Relacatib) Reduces Biomarkers of Bone Resorption Both in Vitro and in an Acute Model of Elevated Bone Turnover in Vivo in Monkeys.Bone. 2007 Jan;40(1):122-31. [Content Brief]
Keywords
