TH-237A(meso-GS 164) is a novel neuroprotective agent exhibiting favorable permeation across the blood brain barrier.IC50 value: 5 nM (EC50, concentration that leads to a 50% increase in neuronal survival in the presence of the Aβ peptides)Target: Primary neurons were isolated from embryonic Sprague-Dawley rats, grown in culture (Michaelis et al., 1994) and exposed to either Aβ25-35 or Aβ1-42 in the presence or absence of TH-237A at concentrations ranging from 0.5 to 60 nM. The neurons were treated with TH-237A for 2 hours prior to exposure to the Aβ peptides. Changes in neuronal survival following treatment with TH 237A were evaluated using the Live/Dead assay. The EC50 for TH-237A was 5 nM, demonstrating that it had excellent neuroprotective properties.
[1]. Kelly E. Desino, Improving Blood Brain Barrier Permeation of Small Molecules Exhibiting Chemotherapeutic and Neuroprotective Effects.