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BRD5814

Chemical Structure : BRD5814

CAS No.: 1953181-29-7

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BRD5814 (BRD-5814;BRD 5814)

Catalog No.: PC-63349Not For Human Use, Lab Use Only.

BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    BRD5814 is a potent, selective, highly brain penetrant β-arrestin biased dopamine D2 receptor (D2R) antagonist with Ki of 0.27 uM.
    BRD5814 strongly diminish D2R/β-arrestin signaling (EC50=0.54 uM) without affecting D2R/Gαi signaling.
    BRD5814 demonstrates good target engagement via PET imaging, achieving efficacy in an amphetamine-induced hyperlocomotion mouse model with strongly reduced motoric side effects in a rotarod performance test.

    Physicochemical Properties

    M.Wt 413.865
    Formula C21H23ClF3NO2
    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-(4-chlorophenoxy)-4-methyl-1-(2-(2-(trifluoromethyl)phenoxy)ethyl)piperidine

    References

    1. Weïwer M, et al. ACS Chem Biol. 2018 Apr 20;13(4):1038-1047.

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