BalicatibBalicatib
MedChemExpress (MCE)
HY-15100
354813-19-7
AAE581
98.00%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.
Balicatib (0-10 µM) shows less than 1.5-fold accumulation of Type I collagen at concentrations up to 10 µM in human dermal fibroblasts[2].
Balicatib (0, 3, 10, 50 mg/kg
Oral gavage
twice daily for 18 months) partially prevented ovariectomyinduced changes in bone mass, inhibited bone turnover at most sites, and had an stimulatory effect on periosteal bone formation in cynomolgus monkeys[1].
cathepsin K 22 nM (IC50) cathepsin L 48 nM (IC50) Cathepsin B 61 nM (IC50) cathepsin S 2900 nM (IC50)
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[1]. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2012 Jan
23(1):339-49. [Content Brief]
[2]. Gauthier JY, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1
18(3):923-8. [Content Brief]