AAE-581


Catalog No. size PriceQuantity
M60434-2S 2mg solid $139
M60434-10S 10mg solid $556

Description

Product Information
Molecular Weight: 411.54
Formula: C23H23N5O2
Purity: >98% 
CAS#: 354813-19-7
Solubility: DMSO: 46 mg/mL
Chemical Name: N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month


Biological Activity:

Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S. IC50 value: Target: cathepsin K The cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.

Reference:

[1]. Falgueyret JP, et al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43.
[2]. Vasiljeva O, et al. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403.
[3]. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2011 Dec;22(12):3001-11.

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