Catalog No.: PC-21108Not For Human Use, Lab Use Only.
CT1812 (Zervimesine) is a potent, orally active dual σ1R and σ2R ligand with Ki of 63 and 8.5 nM respectively, IC50 of 0.31 uM in neuronal trafficking assays.
CT1812 (Zervimesine) is a potent, orally active dual σ1R and σ2R ligand with Ki of 63 and 8.5 nM respectively, IC50 of 0.31 uM in neuronal trafficking assays.
CT1812 prevented and reversed trafficking deficits caused by soluble Aβ oligomers (AβOs), but had no effect in the absence of AβOs in neurons.
CT1812 also prevented binding AβO to neuronal receptors, displaced prebound AβO, and was determined by a one-site ELISA assay to have no effect on AβO assembly or AβO dissociation.
CT1812 is an AβO-displacing compound and a potent and highly selective antagonist of the sigma-2 receptor.
CT1812 significantly increased CSF concentrations of Aβ oligomers in AD patient CSF, reduced concentrations of synaptic proteins and phosphorylated tau fragments, and reversed expression of many AD-related proteins dysregulated in CSF compared to placebo.
