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VU6004256

Chemical Structure : VU6004256

CAS No.: 2011034-33-4

VU6004256 (VU 6004256)

Catalog No.: PC-35486Not For Human Use, Lab Use Only.

VU6004256 (VU 6004256) is a highly potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 155 nM (mouse M1), significant selectivity over M2-M5 (EC50>30 uM).

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    Biological Activity

    VU6004256 (VU 6004256) is a highly potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 155 nM (mouse M1), significant selectivity over M2-M5 (EC50>30 uM).
    VU6004256 normalizes deficits in muscarinic agonist-induced long-term depression in layer V of the PFC in the NR1 KD mice.
    VU6004256 also reduces excessive pyramidal neuron firing in layer V PFC neurons in awake.
    VU6004256 produces a robust, dose-dependent reduction in the hyperlocomotor activity in vivo.

    Physicochemical Properties

    M.Wt 465.505
    Formula C25H25F2N5O2
    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

    4,6-Difluoro-N-[(1S,2S)-2-hydroxycyclohexyl]-1-[[6-(1-methyl-1H-pyrazol-4-yl)-3-pyridinyl]methyl]-1H-indole-3-carboxamide

    References

    1. Grannan MD, et al. ACS Chem Neurosci. 2016 Dec 21;7(12):1706-1716.

    2. Khajehali E, et al. Biochem Pharmacol. 2018 Aug;154:243-254.

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