Relacatib |CAS:362505-84-8 Probechem Biochemicals

Chemical Structure : Relacatib

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Relacatib (SB-462795;GSK-462795)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	540.635
分子式	C27H32N4O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

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.

Relacatib (SB-462795;GSK-462795)

生物&药学活性

物理化学性质&存储条件

参考文献

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Relacatib (SB-462795;GSK-462795)

生物&药学活性

物理化学性质&存储条件

参考文献

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