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UCSF7447

Chemical Structure : UCSF7447

CAS No.: 2305480-97-9

UCSF7447 (UCSF-7447, ZINC555417447)

Catalog No.: PC-38133Not For Human Use, Lab Use Only.

UCSF7447 (UCSF-7447, ZINC555417447) is a potent, selecive, brain permeable melatonin receptor MT-1 inverse agonist with Ki of 304 nM (hMT-1).

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    Biological Activity

    UCSF7447 (UCSF-7447, ZINC555417447) is a potent, selecive, brain permeable melatonin receptor MT-1 inverse agonist with Ki of 304 nM (hMT-1).
    UCSF7447 increased basal cAMP with EC50 value of 41 nM at hMT1, selectivity for hMT1 over hMT2 of 53-fold, and hMT1 inverse agonist efficacies of 62%.
    UCSF7447 advanced the onset of activity by approximately 1 hour at 0.9 μg/mouse (about 0.03 mg/Kg), an effect similar to that of melatonin at its ED50 (0.72 μg/mouse).
    At a higher dose (30 μg/mouse, about 1 mg/Kg), UCSF7447 advanced the onset of running wheel activity with an amplitude similar to melatonin.

    Physicochemical Properties

    M.Wt 363.643
    Formula C15H12BrClN4
    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

    2-Bromo-4-chloro-N-[3-(1H-1,2,4-triazol-5-yl)phenyl]-benzenemethanamine

    References

    1. Reed M Stein, et al. Nature. 2020 Mar;579(7800):609-614.

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