BF 227 is a candidate for an amyloid imaging probe for PET, with a Ki of 4.3 nM for Aβ1-42 fibrils.
BF-227 has a high binding affinity for Aβ1-42 fibrils. The Ki value for Aβ1-42 fibrils in competitive binding assay using [125I]BF-180 is 4.3±1.3 nM in BF-227 (Kd value of [125I]BF-180: 10.8±1.5 nM)[1]. [11C]BF-227 is a PET tracer. The AUC for BF-227 (0.994) is much higher than that for FDG (0.839), indicating that BF-227 is more sensitive as well as more specific than FDG in diagnosing AD[2].
[1]. Kudo Y, et al. Development of amyloid imaging PET probes for an early diagnosis of Alzheimer's disease. Minim Invasive Ther Allied Technol. 2006;15(4):209-13. [2]. Furukawa K, et al. Amyloid PET in mild cognitive impairment and Alzheimer's disease with BF-227: comparison to FDG-PET. J Neurol. 2010 May;257(5):721-7.