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HTL9936

Chemical Structure : HTL9936

CAS No.: 1438242-59-1

HTL9936 (HTL-9936)

Catalog No.: PC-72655Not For Human Use, Lab Use Only.

HTL9936 (HTL-9936) is a potent, selective M1-muscarinic acetylcholine (M1) receptor partial agonist with EC50 of 32 nM.

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    Biological Activity

    HTL9936 (HTL-9936) is a potent, selective M1-muscarinic acetylcholine (M1) receptor partial agonist with EC50 of 32 nM.
    HTL9936 dispalys little to no activity against M2 (EC50>20 uM), M3 (EC50>20 uM), M4 (EC50=398 nM).
    HTL9936 demonstrated agonist activity in pERK1/2 (EC50=32 nM), label-free dynamic mass redistribution (EC50=79 nM) and inositol phosphate (IP1) assay formats (EC5=631 nM) in CHO cells overexpressing human M1-receptor.
    HTL9936 demonstrated no detectable agonism at human M2-, M3-, or M5-receptors, although partial agonist activity was observed at the human M4-receptor.
    Co-administration of HTL9936 with scopolamine resulted in a dose-dependent restoration of learning and memory responses, reverses cognitive deficits in a mouse model of neurodegeneration.

    Physicochemical Properties

    M.Wt 365.518
    Formula C20H35N3O3
    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

    ethyl (S)-4-(4-((1-methylcyclobutyl)carbamoyl)piperidin-1-yl)azepane-1-carboxylate

    References

    1. Alastair J H Brown, et al. Cell. 2021 Nov 24;184(24):5886-5901.e22.

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