XAP044 | mGlu7 antagonist | Probechem Biochemicals

Chemical Structure : XAP044

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XAP044 (XAP-044)

货号: PC-22270Not For Human Use, Lab Use Only.

XAP044 is a potent, selective antagonist of metabotropic glutamate receptor subtype 7 (mGlu7), inhibits lateral amygdala long term potentiation (LTP) in brain slices with IC50 of 88 nM.

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生物&药学活性

XAP044 is a potent, selective antagonist of metabotropic glutamate receptor subtype 7 (mGlu7), inhibits lateral amygdala long term potentiation (LTP) in brain slices with IC50 of 88 nM.
XAP044 binds within the Venus flytrap domain (VFTD) close to the binding site of the orthosteric agonist l-glutamate.
XAP044 selectively and dose-dependently reduced DL-AP4-induced (4 mm) activation of human mGlu7b with IC50 of 2.8 uM, with no effect on DL-AP4-induced activation of [35S]GTPγS binding by mGlu4 and mGlu6 or on GABA-induced (50 μm) activation of [35S]GTPγS binding by GABAB receptors.
XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms. XAP044 reduces freezing during acquisition of Pavlovian fear and reduces innate anxiety.

物理化学性质&存储条件

分子量	380.14
分子式	C15H9IO4
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	7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one

参考文献

1. Gee CE, et al. J Biol Chem. 2014 Apr 18;289(16):10975-10987.

2. Palazzo E, et al. Pain. 2015 Jun;156(6):1060-1073.

XAP044 (XAP-044)

生物&药学活性

物理化学性质&存储条件

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XAP044 (XAP-044)

生物&药学活性

物理化学性质&存储条件

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