Background:

WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay.

WAY-262611 has the most potent activity in the primary assay, low kinase inhibition potential, and high solubility[1].

WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration. Calvariae from wt mice treated with WAY-262611 shows statistically increased BFR, while similarly treated KO animals are no different from control. This indicates that WAY-262611 is acting via the Wnt β-catenin pathway and most likely through inhibition of Dkk-1[1].

参考文献:
[1]. Pelletier JC, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J Med Chem. 2009 Nov 26;52(22):6962-5.