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Barbadin

Chemical Structure : Barbadin

CAS No.: 356568-70-2

Barbadin

Catalog No.: PC-61188Not For Human Use, Lab Use Only.

Barbadin is a small molecule that selectively inhibits the β-arrestin/β2-adaptin interaction (IC50=19.1/15.6 uM for β-arrestin1/2) without effect on the formation of receptor/β-arrestin complexes.

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    Biological Activity

    Barbadin is a small molecule that selectively inhibits the β-arrestin/β2-adaptin interaction (IC50=19.1/15.6 uM for β-arrestin1/2) without effect on the formation of receptor/β-arrestin complexes; selectively inhibits the β-arrestin/AP2 interaction, blocks agonist-promoted endocytosis of the prototypical GPCR β2AR, V2R and AT1R, but does not affect β-arrestin-independent (transferrin) or AP2-independent (endothelin-A) receptor internalization, fully blocks V2R-stimulated ERK1/2 activation and blunts cAMP accumulation promoted by both V2R and β2AR.

    Physicochemical Properties

    M.Wt 333.409
    Formula C19H15N3OS
    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

    3-Azanyl-5-[4-(phenylmethyl)phenyl]thieno[2,3-d]pyrimidin-4-one

    References

    1. Beautrait A, et al. Nat Commun. 2017 Apr 18;8:15054.

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