AT-076 | Pan opioid antagonist | Probechem Biochemicals

Chemical Structure : AT-076

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AT-076 (AT076)

货号: 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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生物&药学活性

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).

物理化学性质&存储条件

分子量	437.58
分子式	C26H35N3O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

AT-076 (AT076)

生物&药学活性

物理化学性质&存储条件

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AT-076 (AT076)

生物&药学活性

物理化学性质&存储条件

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