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首页-小分子抑制剂&激动剂-GPCR-Sigma Receptor-CT1812
CT1812

Chemical Structure : CT1812

CAS No.: 1802632-22-9

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CT1812 (Zervimesine, CT-1812)

货号: 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.

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10 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

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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