Chemical Structure : CT-1812
CAS No.:
1802632-22-9
CT-1812
(CT1812)
Catalog No.: PC-21108Not For Human Use, Lab Use Only.
CT-1812 (CT1812) 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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CT-1812 (CT1812) 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.
CT-1812 prevented and reversed trafficking deficits caused by soluble Aβ oligomers (AβOs), but had no effect in the absence of AβOs in neurons.
CT-1812 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.
CT-1812 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.
Physicochemical Properties
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M.Wt
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431.59
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Formula
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C24H33NO4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-[3-[1,3-Dihydro-5-(methylsulfonyl)-2H-isoindol-2-yl]-3-methylbutyl]-2-(1,1-dimethylethoxy)phenol
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References
1. Izzo NJ, et al. Alzheimers Dement. 2021 Aug;17(8):1365-1382.
2. Rishton GM, et al. ACS Med Chem Lett. 2021 Aug 9;12(9):1389-1395.
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