BF-168

BF-168, a candidate probe for PET, is found to specifically recognize both neuritic and diffuse plaques, with a K_i of 6.4 nM for Aβ1-42. IC50 & Target: Ki: 6.4 nM (Aβ1-42)^[1]. In Vitro: BF-168, a styrylbenzoxazole derivative, is a potent agent that selectively recognizes SPs and NFTs in AD brain. BF-168 is a candidate probe for PET and is found to specifically recognize both neuritic and diffuse plaques, with a K_i of 6.4 nM for Aβ1-42^[1]. In Vivo: Intravenous injection of BF-168 in PS1/APP and APP23 transgenic mice result in specific in vivo labeling to both compact and diffuse amyloid deposits in the brain. In addition, ¹⁸F-radiolabeled BF-168 demonstrates abundant initial brain uptake (3.9% injected dose/gm at 2 min after injection) and fast clearance (t_1/2=24.7 min) after intravenous administration in normal mice. Furthermore, autoradiograms of brain sections from APP23 transgenic mice at 180 min after intravenous injection of [¹⁸F]BF-168 shows selective labeling of brain amyloid deposits with little nonspecific binding^[1].