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AT-076

Chemical Structure : AT-076

CAS No.: 1657028-64-2

AT-076 (AT076)

Catalog No.: PC-20510Not For Human Use, Lab Use Only.

AT-076 (AT076) is the first potent small-molecule opioid pan antagonist with receptor binding Ki values of 1.75, 1.14, 1.67 and 19.6 nM for NOP, KOP, MOP, and DOP, respectively.

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

    Biological Activity

    AT-076 (AT076) is the first potent small-molecule opioid pan antagonist with receptor binding Ki values of 1.75, 1.14, 1.67 and 19.6 nM for NOP, KOP, MOP, and DOP, respectively.
    AT-076 demonstrates Ke values of 0.58 and 24.95 nM for inhibition of agonist-stimulated [35S]GTPγS binding curves.
    AT-076 shows that it has a noncompetitive antagonist profile at the NOP and KOP receptors (insurmountable antagonism), but is a potent competitive antagonist at the MOP and DOP receptors, with Ke values 3–6-fold more potent than those of JDTic (Cat. PC-42614).

    Physicochemical Properties

    M.Wt 437.58
    Formula C26H35N3O3
    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

    (R)-7-hydroxy-N-((S)-1-(4-(3-hydroxyphenyl)piperidin-1-yl)-3-methylbutan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide

    References

    1. Zaveri NT, et al. ACS Chem Neurosci. 2015 Apr 15;6(4):646-57.

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