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首页-小分子抑制剂&激动剂-GPCR-Sigma Receptor-CT-1812
CT-1812

Chemical Structure : CT-1812

CAS No.: 1802632-22-9

CT-1812 (CT1812)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 431.59
分子式 C24H33NO4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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