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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)

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

O=C([C@@H]1NCC2=C(C=CC(O)=C2)C1)N[C@@H](C(C)C)CN3CCC(C4=CC=CC(O)=C4)CC3

References

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

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