FPS-ZM1

A high-affinity RAGE (Receptor for Advanced Glycation End products) receptor antagonist (Ki = 25 nM). It lowers levels of Aβ via binding to the V domain of RAGE and can block multiple mechanisms of Aβ40- and Aβ42-induced cellular stress in RAGE-expressing brain endothelium, neurons and microglia in vitro and in vivo (1,2). In a rat model of intracerebral hemorrhage, FPS-ZM1 attenuates blood-brain barrier and white matter fiber damage (3). It ameliorates inflammatory damage after acute intracerebral hemorrhage via downstream blockade of high mobility box-1(HMGB1) signaling (4). Attenuates AGE-induced neuroinflammation and oxidative stress in rat microglia (5). BBB permeable.

1. R Deane et al. J. Clin. Invest. 2012 122:1377 2. Y Hong et al. Neurochem. Res. 2016 41:1192 3. F Yang et al. Stroke 2015 46:1328 4. D Li et al. Neurosci. Lett. 2015 609:109 5. C Shen et al. Neurochem. Res. 2017 June 29 epub