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SAS-0132

Chemical Structure : SAS-0132

CAS No.: 2095551-89-4

SAS-0132 (SAS 0132;SAS0132;SAS 132)

Catalog No.: PC-61100Not For Human Use, Lab Use Only.

SAS-0132 (SAS132) is a novel potent, subtype-selective, brain penetrant sigma 2 receptor/PGRMC1 ligand with Ki of 90 nM, 9-fold selectivity over sigma 1 receptors.

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    Biological Activity

    SAS-0132 (SAS132) is a novel potent, subtype-selective, brain penetrant sigma 2 receptor/PGRMC1 ligand with Ki of 90 nM, 9-fold selectivity over sigma 1 receptors.
    SAS-0132 also exhibits low off-target affinity for most CNS-relevant targets, including opioid, adrenergic, nACR, mAChR, and NMDA receptors.
    SAS-0132 modulates intracellular Ca2+ levels in human SK-N-SH neuroblastoma cells, and is neuroprotective in a C. elegans model of amyloid precursor protein-mediated neurodegeneration, improves cognitive performance in transgenic mouse model of AD.

    Physicochemical Properties

    M.Wt 391.515
    Formula C24H29N3O2
    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

    benzyl (1R,5S)-8-(4-methylpiperazin-1-yl)-1,3,4,5-tetrahydro-2H-1,5-methanobenzo[c]azepine-2-carboxylate

    References

    1. Yi B, et al. J Neurochem. 2017 Feb;140(4):561-575.

    2. Sahn JJ, et al. ACS Chem Neurosci. 2017 Aug 16;8(8):1801-1811.

    3. Sahn JJ, et al. ChemMedChem. 2016 Mar 17;11(6):556-61.

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