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Chemical Structure : XAP044
Catalog No.: 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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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.
| M.Wt | 380.14 | |
| Formula | C15H9IO4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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