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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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
|
M.Wt
|
431.59
|
|
Formula
|
C24H33NO4S
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
4-[3-[1,3-Dihydro-5-(methylsulfonyl)-2H-isoindol-2-yl]-3-methylbutyl]-2-(1,1-dimethylethoxy)phenol
|
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.
Contact Us
sales@probechem.com
